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Book
Synthesis of Flavonoids or Other Nature-Inspired Small Molecules
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Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

This Special Issue aims to provide an updated overview of the flourishing ongoing research activity in the field of the chemistry of natural and nature-inspired compounds. Ten of the submitted articles were accepted for publication after peer-review. Interestingly, the published papers cover a wide range of chemical reactions, different scaffolds, and several medicinal chemistry applications. Moreover, this Special Issue gathered contributions from all over the world, testifying the international scientific community’s interest in this topic. I would like to sincerely thank the MDPI staff, particularly Jade Lu and the editorial team of Molbank. I am particularly grateful to the authors that decided to share the results of their research by contributing their manuscript to this Special Issue, and, of course, to the reviewers for their valuable help.

Keywords

Research & information: general --- quercetin --- flavonoids --- semi-synthetic --- PDE --- sildenafil --- molecular modeling --- Garcinia porrecta --- Clusiaceae --- xanthone --- Lansium domesticum --- Meliaceae --- MCF-7 --- triterpene onoceranoid --- hydrazone --- (+)-camphor --- valproic acid --- technology --- terpenoid --- anticonvulsant activity --- 1,2,3-triazole --- anticancer --- aminoquinoline --- hybrid compound --- kokosanolide --- tetranortriterpenoid --- C. dichotoma --- antidiabetic --- α-glucosidase --- α-amylase --- docking --- ADMET --- curcumin analog --- organic synthesis --- photophysical properties --- steady-state fluorescence --- DFT calculation --- 7-hydroxy-2H-chromen-2-one --- O-acylation reaction --- coumarin --- lupeol derivative --- benzylidene derivative --- α-glucosidase inhibition --- Oxone® --- quercetin --- flavonoids --- semi-synthetic --- PDE --- sildenafil --- molecular modeling --- Garcinia porrecta --- Clusiaceae --- xanthone --- Lansium domesticum --- Meliaceae --- MCF-7 --- triterpene onoceranoid --- hydrazone --- (+)-camphor --- valproic acid --- technology --- terpenoid --- anticonvulsant activity --- 1,2,3-triazole --- anticancer --- aminoquinoline --- hybrid compound --- kokosanolide --- tetranortriterpenoid --- C. dichotoma --- antidiabetic --- α-glucosidase --- α-amylase --- docking --- ADMET --- curcumin analog --- organic synthesis --- photophysical properties --- steady-state fluorescence --- DFT calculation --- 7-hydroxy-2H-chromen-2-one --- O-acylation reaction --- coumarin --- lupeol derivative --- benzylidene derivative --- α-glucosidase inhibition --- Oxone®


Book
Synthesis of Flavonoids or Other Nature-Inspired Small Molecules
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Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

This Special Issue aims to provide an updated overview of the flourishing ongoing research activity in the field of the chemistry of natural and nature-inspired compounds. Ten of the submitted articles were accepted for publication after peer-review. Interestingly, the published papers cover a wide range of chemical reactions, different scaffolds, and several medicinal chemistry applications. Moreover, this Special Issue gathered contributions from all over the world, testifying the international scientific community’s interest in this topic. I would like to sincerely thank the MDPI staff, particularly Jade Lu and the editorial team of Molbank. I am particularly grateful to the authors that decided to share the results of their research by contributing their manuscript to this Special Issue, and, of course, to the reviewers for their valuable help.


Book
Synthesis of Flavonoids or Other Nature-Inspired Small Molecules
Author:
Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

This Special Issue aims to provide an updated overview of the flourishing ongoing research activity in the field of the chemistry of natural and nature-inspired compounds. Ten of the submitted articles were accepted for publication after peer-review. Interestingly, the published papers cover a wide range of chemical reactions, different scaffolds, and several medicinal chemistry applications. Moreover, this Special Issue gathered contributions from all over the world, testifying the international scientific community’s interest in this topic. I would like to sincerely thank the MDPI staff, particularly Jade Lu and the editorial team of Molbank. I am particularly grateful to the authors that decided to share the results of their research by contributing their manuscript to this Special Issue, and, of course, to the reviewers for their valuable help.


Book
Synthesis and Applications of New Spin Crossover Compounds
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ISBN: 3039213628 303921361X Year: 2019 Publisher: MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

The crystal chemistry of spin crossover (SCO) behavior in coordination compounds can potentially be in association with smart materials—promising materials for applications as components of memory devices, displays, sensors and mechanical devices and, especially, actuators, such as artificial muscles. This Special Issue is devoted to various aspects of SCO and related research, comprising 18 interesting original papers on valuable and important SCO topics. Significant and fundamental scientific attention has been focused on the SCO phenomena in a wide research range of fields of fundamental chemical and physical and related sciences, containing the interdisciplinary regions of chemical and physical sciences related to the SCO phenomena. Coordination materials with bistable systems between the LS and the HS states are usually triggered by external stimuli, such as temperature, light, pressure, guest molecule inclusion, soft X-ray, and nuclear decay. Since the first Hofmann-like spin crossover (SCO) behavior in {Fe(py)2[Ni(CN)4]}n (py = pyridine) was demonstrated, this crystal chemistry motif has been frequently used to design Fe(II) SCO materials to enable determination of the correlations between structural features and magnetic properties.

Keywords

n/a --- hexadentate ligand --- X-ray diffraction --- structural disorder --- lattice energy --- 2-bis(4-pyridyl)ethane --- thermal hysteresis --- optical conductivity spectrum --- spin-state crossover --- solvate --- single crystal --- spin-crossover transition --- spin-crossover --- cobalt oxide --- amorphous --- metal dithiolene complexes --- qsal ligand --- impurity effect --- 3-triazole --- intermolecular interactions --- spin crossover --- hydrogen bonding --- 1 --- 2 --- optical microscopy --- supramolecular coordination polymer --- paramagnetic ligand --- magnetic susceptibility --- high spin --- [Fe(III)(3-OMesal2-trien)]+ --- aminoxyl --- cobalt(II) ion --- mosaicity --- Fe(III) coordination complexes --- nitroxides --- C–H···? interactions --- Fe(II) --- dithiooxalato ligand --- dinuclear triple helicate --- coordination polymers --- magnetization --- spiral structure --- magnetostructural correlations --- charge-transfer phase transition --- structure phase transition --- magnetic properties --- spin polaron --- substitution of 3d transition metal ion --- iron(II) complexes --- X-ray absorption spectroscopy --- coordination complexes --- crystal engineering --- fatigability --- soft X-ray induced excited spin state trapping --- spin transition --- dipyridyl-N-alkylamine ligands --- coordination polymer --- iron (II) --- iron mixed-valence complex --- chiral propeller structure --- spin cross-over (SCO) --- EPR spectroscopy --- Cu(II) complexes --- solvent effects --- ferromagnetism --- SQUID --- LIESST effect --- low spin (LS) --- 57Fe Mössbauer spectroscopy --- dielectric response --- iron(II) --- hetero metal complex --- atropisomerism --- switch --- Schiff base --- counter-anion --- DFT calculation --- Fe(III) complex --- Fe(II) complex --- high spin (HS) --- reaction diffusion --- thermochromism --- supramolecular isomerism --- phase transition --- magnetic transition --- mononuclear --- [Au(dmit)2]? --- UV-Vis spectroscopy --- phase transitions --- ?-? interactions --- [Au(dddt)2]? --- crystal structure --- linear pentadentate ligand --- ion-pair crystals --- C-H···? interactions --- 57Fe Mössbauer spectroscopy


Book
Anticancer Agents : Design, Synthesis and Evaluation
Author:
Year: 2021 Publisher: Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute

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This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers.

Keywords

Medicine --- benzofurans --- chemical synthesis --- cytotoxic properties --- HeLa --- MOLT-4 --- K562 --- anticancer --- anti-neuroinflammation --- coumarin --- dihydroartemisinin --- flavonoids --- allene --- E-stereoselective --- regioselective --- anti-cancer activity --- cyanopyridone --- substituted pyridine --- pyridotriazine --- pyrazolopyridine --- thioxotriazopyridine --- anticancer activity --- HepG2 --- antitumor activity --- computational docking --- MDM2-p53 interaction --- xanthones --- yeast-based assays --- estrone derivatives --- hydrazine --- N-substituted pyrazoline --- anti-ovarian cancer --- topoisomerase II inhibitor --- kinase inhibitor --- antiproliferative agent --- urea --- synthesis --- antiproliferative activity --- apoptosis --- indoleamine 2,3-dioxygenase --- inhibitor --- anti-tumor --- immune modulation --- tryptophan metabolism --- taxoids --- βIII-tubulin --- P-glycoprotein --- drug resistance --- thiopene --- thienopyrimidinone --- thiazolidinone --- breast cancer --- benzofuran–pyrazole --- nanoparticles --- cytotoxic activity --- PARP-1 inhibition --- 3,6-dibromocarbazole --- 5-bromoindole --- carbazole --- actin --- migration --- Thienopyrimidine --- Pyrazole --- PI3Kα inhibitor --- quinazolin-4(3H)-one --- quinazolin-4(3H)-thione --- Schiff base --- antioxidant activity --- DFT study --- ortho-quinones --- beta-lapachone --- tanshione IIA --- PI3Ks --- PI3Kδ inhibitors --- 2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide --- anticancer agents --- protein–protein interactions --- virtual screening --- mimetics --- drug discovery --- bivalency --- polyvalency --- antitumor --- cell cycle --- ovarian cancer --- P-MAPA --- IL-12 --- TLR signaling --- inflammation --- chemoresistance --- 4-(pyridin-4-yloxy)benzamide --- 1,2,3-triazole --- c-Met --- natural product --- anticancer agent --- zampanolide --- Talazoparib --- PARP inhibitor --- prodrug --- o-nitro-benzyl --- photoactivatable protecting groups --- salinomycin --- overcoming drug resistance --- tumor specificity --- synergy --- 5-fluorouracil --- gemcitabine --- amides/esters --- colchicine analogs --- thiocolchicine --- colchiceine --- antimitotic agents --- hydrates --- dihydropyranoindole --- HDAC inhibitors --- neuroblastoma --- aromatase --- MCF-7 --- NIH3T3 --- benzimidazole --- triazolothiadiazine --- docking --- ADME --- organosilicon compounds --- SILA-409 (Alis-409) --- SILA-421 (Alis-421) --- multidrug resistance (MDR) reversal --- ABCB1 (P-glycoprotein) --- colon cancer --- colchicine amide --- colchicine sulfonamide --- tubulin inhibitors --- docking studies --- crystal structure --- PROTACs --- protein degradation --- IGF-1R --- Src --- protein kinase --- phenylpyrazolopyrimidine --- enzyme inhibition --- molecular simulation --- androgen receptor --- prostate cancer --- enzalutamide --- apalutamide --- darolutamide --- triple-negative breast cancer --- cytotoxicity --- chrysin analogues --- flavonoid --- anticancer compounds --- benzofurans --- chemical synthesis --- cytotoxic properties --- HeLa --- MOLT-4 --- K562 --- anticancer --- anti-neuroinflammation --- coumarin --- dihydroartemisinin --- flavonoids --- allene --- E-stereoselective --- regioselective --- anti-cancer activity --- cyanopyridone --- substituted pyridine --- pyridotriazine --- pyrazolopyridine --- thioxotriazopyridine --- anticancer activity --- HepG2 --- antitumor activity --- computational docking --- MDM2-p53 interaction --- xanthones --- yeast-based assays --- estrone derivatives --- hydrazine --- N-substituted pyrazoline --- anti-ovarian cancer --- topoisomerase II inhibitor --- kinase inhibitor --- antiproliferative agent --- urea --- synthesis --- antiproliferative activity --- apoptosis --- indoleamine 2,3-dioxygenase --- inhibitor --- anti-tumor --- immune modulation --- tryptophan metabolism --- taxoids --- βIII-tubulin --- P-glycoprotein --- drug resistance --- thiopene --- thienopyrimidinone --- thiazolidinone --- breast cancer --- benzofuran–pyrazole --- nanoparticles --- cytotoxic activity --- PARP-1 inhibition --- 3,6-dibromocarbazole --- 5-bromoindole --- carbazole --- actin --- migration --- Thienopyrimidine --- Pyrazole --- PI3Kα inhibitor --- quinazolin-4(3H)-one --- quinazolin-4(3H)-thione --- Schiff base --- antioxidant activity --- DFT study --- ortho-quinones --- beta-lapachone --- tanshione IIA --- PI3Ks --- PI3Kδ inhibitors --- 2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide --- anticancer agents --- protein–protein interactions --- virtual screening --- mimetics --- drug discovery --- bivalency --- polyvalency --- antitumor --- cell cycle --- ovarian cancer --- P-MAPA --- IL-12 --- TLR signaling --- inflammation --- chemoresistance --- 4-(pyridin-4-yloxy)benzamide --- 1,2,3-triazole --- c-Met --- natural product --- anticancer agent --- zampanolide --- Talazoparib --- PARP inhibitor --- prodrug --- o-nitro-benzyl --- photoactivatable protecting groups --- salinomycin --- overcoming drug resistance --- tumor specificity --- synergy --- 5-fluorouracil --- gemcitabine --- amides/esters --- colchicine analogs --- thiocolchicine --- colchiceine --- antimitotic agents --- hydrates --- dihydropyranoindole --- HDAC inhibitors --- neuroblastoma --- aromatase --- MCF-7 --- NIH3T3 --- benzimidazole --- triazolothiadiazine --- docking --- ADME --- organosilicon compounds --- SILA-409 (Alis-409) --- SILA-421 (Alis-421) --- multidrug resistance (MDR) reversal --- ABCB1 (P-glycoprotein) --- colon cancer --- colchicine amide --- colchicine sulfonamide --- tubulin inhibitors --- docking studies --- crystal structure --- PROTACs --- protein degradation --- IGF-1R --- Src --- protein kinase --- phenylpyrazolopyrimidine --- enzyme inhibition --- molecular simulation --- androgen receptor --- prostate cancer --- enzalutamide --- apalutamide --- darolutamide --- triple-negative breast cancer --- cytotoxicity --- chrysin analogues --- flavonoid --- anticancer compounds


Book
Anticancer Drugs 2021
Authors: ---
Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

The Special Issue "Anticancer Drugs 2021" of Pharmaceuticals is focused on recent significant advances in the design, synthesis, molecular mechanism of action and therapeutic applications of anticancer drugs. This collection of preclinical research papers and reviews includes designed chemotherapeutic agents, targeted therapies and biological agents. The rationalization for the biological activity of these drugs is presented, which helps to guide the design of more effective agents. Structure–activity relationships, together with the biological context in which targets are selected for oncology drug development, are also considered.

Keywords

Research & information: general --- Chemistry --- thymidylate synthase --- cytotoxicity --- 1,2,3-triazole --- 1,3,4-oxadiazole --- 5-fluoruracil --- pemetrexed --- docking --- 3,4'-bis-guanidino --- 3-amino-4'-guanidino --- diphenyl ether --- phenyl pyridyl ether --- intramolecular hydrogen bond --- cancer cell viability --- HL-60 --- BRAF --- apoptosis --- thieno[2,3-d][1,2,3]triazine --- acetamide --- H1299 --- HER2 --- EGFR --- Bcl-2 inhibitors --- Indole-based analogues --- benzimidazole --- MTT cytotoxic assay --- cell cycle analysis --- DNA fragmentation --- ELISA --- solid/lipid nanoparticles --- phenstatin --- letrozole --- tubulin polymerisation inhibitor --- aromatase inhibitor --- breast cancer --- hybrid molecule --- dual-targeting molecule --- designed multiple ligand --- NaMSA --- cyclophosphamide --- histopathology --- testis --- urinary bladder --- anticancer agents --- enantioselective synthesis --- gastric adenocarcinoma --- tryptophanol --- concentration-guided dosing --- model informed dosing --- physiologically based pharmacokinetics --- sorafenib --- tyrosil-DNA-phosphodiesterase 1 --- adamantane --- resin acid --- TDP1 --- cytotoxic agents --- apoptosis induction --- HT-29 cells --- MDA-MB-231 cells --- mechanism prediction --- STAT inhibitors --- miR-21 --- hydrazide derivatives --- nitrogen scaffolds --- mitoxantrone --- cardiotoxicity --- inflammation --- oxidative stress --- age --- cumulative dose --- Trk --- NTRK --- tissue-agnostic --- larotrectinib --- entrectinib --- Trk fusion --- protein kinase inhibitors --- USFDA --- cancer --- patent review --- generic product --- doxazosin --- MD simulations --- combretastatin A-4 --- cytotoxic activity --- hybrid compounds --- indazole --- mucin --- MUC1 --- MUC16 --- immunotherapy --- cancer vaccine --- CAR (chimeric antigen receptor) --- ADC (antibody-drug conjugate) --- thiourea --- interleukin-6 --- trypan blue assay --- chalcones --- exportin-1 --- covalent binding --- CovDock --- anticancer activity --- xanthone --- in vitro --- in vivo --- isolation --- synthesis --- heterocyclic compound --- benzenesulfonamides --- imidazoles --- alkylated --- colony formation --- tumor spheroids --- HDAC inhibitors --- chalcone --- dual inhibitors --- carvedilol --- kidney --- toxicity --- 7-deaza-4'-thioadenosine derivatives --- multi-kinase inhibitor --- anticancer --- nucleoside --- Imiquimod --- drug efflux --- multidrug resistance --- Toll-Like Receptor --- thymidylate synthase --- cytotoxicity --- 1,2,3-triazole --- 1,3,4-oxadiazole --- 5-fluoruracil --- pemetrexed --- docking --- 3,4'-bis-guanidino --- 3-amino-4'-guanidino --- diphenyl ether --- phenyl pyridyl ether --- intramolecular hydrogen bond --- cancer cell viability --- HL-60 --- BRAF --- apoptosis --- thieno[2,3-d][1,2,3]triazine --- acetamide --- H1299 --- HER2 --- EGFR --- Bcl-2 inhibitors --- Indole-based analogues --- benzimidazole --- MTT cytotoxic assay --- cell cycle analysis --- DNA fragmentation --- ELISA --- solid/lipid nanoparticles --- phenstatin --- letrozole --- tubulin polymerisation inhibitor --- aromatase inhibitor --- breast cancer --- hybrid molecule --- dual-targeting molecule --- designed multiple ligand --- NaMSA --- cyclophosphamide --- histopathology --- testis --- urinary bladder --- anticancer agents --- enantioselective synthesis --- gastric adenocarcinoma --- tryptophanol --- concentration-guided dosing --- model informed dosing --- physiologically based pharmacokinetics --- sorafenib --- tyrosil-DNA-phosphodiesterase 1 --- adamantane --- resin acid --- TDP1 --- cytotoxic agents --- apoptosis induction --- HT-29 cells --- MDA-MB-231 cells --- mechanism prediction --- STAT inhibitors --- miR-21 --- hydrazide derivatives --- nitrogen scaffolds --- mitoxantrone --- cardiotoxicity --- inflammation --- oxidative stress --- age --- cumulative dose --- Trk --- NTRK --- tissue-agnostic --- larotrectinib --- entrectinib --- Trk fusion --- protein kinase inhibitors --- USFDA --- cancer --- patent review --- generic product --- doxazosin --- MD simulations --- combretastatin A-4 --- cytotoxic activity --- hybrid compounds --- indazole --- mucin --- MUC1 --- MUC16 --- immunotherapy --- cancer vaccine --- CAR (chimeric antigen receptor) --- ADC (antibody-drug conjugate) --- thiourea --- interleukin-6 --- trypan blue assay --- chalcones --- exportin-1 --- covalent binding --- CovDock --- anticancer activity --- xanthone --- in vitro --- in vivo --- isolation --- synthesis --- heterocyclic compound --- benzenesulfonamides --- imidazoles --- alkylated --- colony formation --- tumor spheroids --- HDAC inhibitors --- chalcone --- dual inhibitors --- carvedilol --- kidney --- toxicity --- 7-deaza-4'-thioadenosine derivatives --- multi-kinase inhibitor --- anticancer --- nucleoside --- Imiquimod --- drug efflux --- multidrug resistance --- Toll-Like Receptor


Book
Anticancer Agents : Design, Synthesis and Evaluation
Author:
Year: 2021 Publisher: Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers.

Keywords

Medicine --- benzofurans --- chemical synthesis --- cytotoxic properties --- HeLa --- MOLT-4 --- K562 --- anticancer --- anti-neuroinflammation --- coumarin --- dihydroartemisinin --- flavonoids --- allene --- E-stereoselective --- regioselective --- anti-cancer activity --- cyanopyridone --- substituted pyridine --- pyridotriazine --- pyrazolopyridine --- thioxotriazopyridine --- anticancer activity --- HepG2 --- antitumor activity --- computational docking --- MDM2-p53 interaction --- xanthones --- yeast-based assays --- estrone derivatives --- hydrazine --- N-substituted pyrazoline --- anti-ovarian cancer --- topoisomerase II inhibitor --- kinase inhibitor --- antiproliferative agent --- urea --- synthesis --- antiproliferative activity --- apoptosis --- indoleamine 2,3-dioxygenase --- inhibitor --- anti-tumor --- immune modulation --- tryptophan metabolism --- taxoids --- βIII-tubulin --- P-glycoprotein --- drug resistance --- thiopene --- thienopyrimidinone --- thiazolidinone --- breast cancer --- benzofuran–pyrazole --- nanoparticles --- cytotoxic activity --- PARP-1 inhibition --- 3,6-dibromocarbazole --- 5-bromoindole --- carbazole --- actin --- migration --- Thienopyrimidine --- Pyrazole --- PI3Kα inhibitor --- quinazolin-4(3H)-one --- quinazolin-4(3H)-thione --- Schiff base --- antioxidant activity --- DFT study --- ortho-quinones --- beta-lapachone --- tanshione IIA --- PI3Ks --- PI3Kδ inhibitors --- 2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide --- anticancer agents --- protein–protein interactions --- virtual screening --- mimetics --- drug discovery --- bivalency --- polyvalency --- antitumor --- cell cycle --- ovarian cancer --- P-MAPA --- IL-12 --- TLR signaling --- inflammation --- chemoresistance --- 4-(pyridin-4-yloxy)benzamide --- 1,2,3-triazole --- c-Met --- natural product --- anticancer agent --- zampanolide --- Talazoparib --- PARP inhibitor --- prodrug --- o-nitro-benzyl --- photoactivatable protecting groups --- salinomycin --- overcoming drug resistance --- tumor specificity --- synergy --- 5-fluorouracil --- gemcitabine --- amides/esters --- colchicine analogs --- thiocolchicine --- colchiceine --- antimitotic agents --- hydrates --- dihydropyranoindole --- HDAC inhibitors --- neuroblastoma --- aromatase --- MCF-7 --- NIH3T3 --- benzimidazole --- triazolothiadiazine --- docking --- ADME --- organosilicon compounds --- SILA-409 (Alis-409) --- SILA-421 (Alis-421) --- multidrug resistance (MDR) reversal --- ABCB1 (P-glycoprotein) --- colon cancer --- colchicine amide --- colchicine sulfonamide --- tubulin inhibitors --- docking studies --- crystal structure --- PROTACs --- protein degradation --- IGF-1R --- Src --- protein kinase --- phenylpyrazolopyrimidine --- enzyme inhibition --- molecular simulation --- androgen receptor --- prostate cancer --- enzalutamide --- apalutamide --- darolutamide --- triple-negative breast cancer --- cytotoxicity --- chrysin analogues --- flavonoid --- anticancer compounds


Book
Anticancer Drugs 2021
Authors: ---
Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

The Special Issue "Anticancer Drugs 2021" of Pharmaceuticals is focused on recent significant advances in the design, synthesis, molecular mechanism of action and therapeutic applications of anticancer drugs. This collection of preclinical research papers and reviews includes designed chemotherapeutic agents, targeted therapies and biological agents. The rationalization for the biological activity of these drugs is presented, which helps to guide the design of more effective agents. Structure–activity relationships, together with the biological context in which targets are selected for oncology drug development, are also considered.

Keywords

Research & information: general --- Chemistry --- thymidylate synthase --- cytotoxicity --- 1,2,3-triazole --- 1,3,4-oxadiazole --- 5-fluoruracil --- pemetrexed --- docking --- 3,4′-bis-guanidino --- 3-amino-4′-guanidino --- diphenyl ether --- phenyl pyridyl ether --- intramolecular hydrogen bond --- cancer cell viability --- HL-60 --- BRAF --- apoptosis --- thieno[2,3-d][1,2,3]triazine --- acetamide --- H1299 --- HER2 --- EGFR --- Bcl-2 inhibitors --- Indole-based analogues --- benzimidazole --- MTT cytotoxic assay --- cell cycle analysis --- DNA fragmentation --- ELISA --- solid/lipid nanoparticles --- phenstatin --- letrozole --- tubulin polymerisation inhibitor --- aromatase inhibitor --- breast cancer --- hybrid molecule --- dual-targeting molecule --- designed multiple ligand --- NaMSA --- cyclophosphamide --- histopathology --- testis --- urinary bladder --- anticancer agents --- enantioselective synthesis --- gastric adenocarcinoma --- tryptophanol --- concentration-guided dosing --- model informed dosing --- physiologically based pharmacokinetics --- sorafenib --- tyrosil-DNA-phosphodiesterase 1 --- adamantane --- resin acid --- TDP1 --- cytotoxic agents --- apoptosis induction --- HT-29 cells --- MDA-MB-231 cells --- mechanism prediction --- STAT inhibitors --- miR-21 --- hydrazide derivatives --- nitrogen scaffolds --- mitoxantrone --- cardiotoxicity --- inflammation --- oxidative stress --- age --- cumulative dose --- Trk --- NTRK --- tissue-agnostic --- larotrectinib --- entrectinib --- Trk fusion --- protein kinase inhibitors --- USFDA --- cancer --- patent review --- generic product --- doxazosin --- MD simulations --- combretastatin A-4 --- cytotoxic activity --- hybrid compounds --- indazole --- mucin --- MUC1 --- MUC16 --- immunotherapy --- cancer vaccine --- CAR (chimeric antigen receptor) --- ADC (antibody-drug conjugate) --- thiourea --- interleukin-6 --- trypan blue assay --- chalcones --- exportin-1 --- covalent binding --- CovDock --- anticancer activity --- xanthone --- in vitro --- in vivo --- isolation --- synthesis --- heterocyclic compound --- benzenesulfonamides --- imidazoles --- alkylated --- colony formation --- tumor spheroids --- HDAC inhibitors --- chalcone --- dual inhibitors --- carvedilol --- kidney --- toxicity --- 7-deaza-4′-thioadenosine derivatives --- multi-kinase inhibitor --- anticancer --- nucleoside --- Imiquimod --- drug efflux --- multidrug resistance --- Toll-Like Receptor --- n/a --- 3,4'-bis-guanidino --- 3-amino-4'-guanidino --- 7-deaza-4'-thioadenosine derivatives


Book
Anticancer Agents : Design, Synthesis and Evaluation
Author:
Year: 2021 Publisher: Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers.

Keywords

benzofurans --- chemical synthesis --- cytotoxic properties --- HeLa --- MOLT-4 --- K562 --- anticancer --- anti-neuroinflammation --- coumarin --- dihydroartemisinin --- flavonoids --- allene --- E-stereoselective --- regioselective --- anti-cancer activity --- cyanopyridone --- substituted pyridine --- pyridotriazine --- pyrazolopyridine --- thioxotriazopyridine --- anticancer activity --- HepG2 --- antitumor activity --- computational docking --- MDM2-p53 interaction --- xanthones --- yeast-based assays --- estrone derivatives --- hydrazine --- N-substituted pyrazoline --- anti-ovarian cancer --- topoisomerase II inhibitor --- kinase inhibitor --- antiproliferative agent --- urea --- synthesis --- antiproliferative activity --- apoptosis --- indoleamine 2,3-dioxygenase --- inhibitor --- anti-tumor --- immune modulation --- tryptophan metabolism --- taxoids --- βIII-tubulin --- P-glycoprotein --- drug resistance --- thiopene --- thienopyrimidinone --- thiazolidinone --- breast cancer --- benzofuran–pyrazole --- nanoparticles --- cytotoxic activity --- PARP-1 inhibition --- 3,6-dibromocarbazole --- 5-bromoindole --- carbazole --- actin --- migration --- Thienopyrimidine --- Pyrazole --- PI3Kα inhibitor --- quinazolin-4(3H)-one --- quinazolin-4(3H)-thione --- Schiff base --- antioxidant activity --- DFT study --- ortho-quinones --- beta-lapachone --- tanshione IIA --- PI3Ks --- PI3Kδ inhibitors --- 2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide --- anticancer agents --- protein–protein interactions --- virtual screening --- mimetics --- drug discovery --- bivalency --- polyvalency --- antitumor --- cell cycle --- ovarian cancer --- P-MAPA --- IL-12 --- TLR signaling --- inflammation --- chemoresistance --- 4-(pyridin-4-yloxy)benzamide --- 1,2,3-triazole --- c-Met --- natural product --- anticancer agent --- zampanolide --- Talazoparib --- PARP inhibitor --- prodrug --- o-nitro-benzyl --- photoactivatable protecting groups --- salinomycin --- overcoming drug resistance --- tumor specificity --- synergy --- 5-fluorouracil --- gemcitabine --- amides/esters --- colchicine analogs --- thiocolchicine --- colchiceine --- antimitotic agents --- hydrates --- dihydropyranoindole --- HDAC inhibitors --- neuroblastoma --- aromatase --- MCF-7 --- NIH3T3 --- benzimidazole --- triazolothiadiazine --- docking --- ADME --- organosilicon compounds --- SILA-409 (Alis-409) --- SILA-421 (Alis-421) --- multidrug resistance (MDR) reversal --- ABCB1 (P-glycoprotein) --- colon cancer --- colchicine amide --- colchicine sulfonamide --- tubulin inhibitors --- docking studies --- crystal structure --- PROTACs --- protein degradation --- IGF-1R --- Src --- protein kinase --- phenylpyrazolopyrimidine --- enzyme inhibition --- molecular simulation --- androgen receptor --- prostate cancer --- enzalutamide --- apalutamide --- darolutamide --- triple-negative breast cancer --- cytotoxicity --- chrysin analogues --- flavonoid --- anticancer compounds


Book
Anticancer Drugs 2021
Authors: ---
Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

The Special Issue "Anticancer Drugs 2021" of Pharmaceuticals is focused on recent significant advances in the design, synthesis, molecular mechanism of action and therapeutic applications of anticancer drugs. This collection of preclinical research papers and reviews includes designed chemotherapeutic agents, targeted therapies and biological agents. The rationalization for the biological activity of these drugs is presented, which helps to guide the design of more effective agents. Structure–activity relationships, together with the biological context in which targets are selected for oncology drug development, are also considered.

Keywords

thymidylate synthase --- cytotoxicity --- 1,2,3-triazole --- 1,3,4-oxadiazole --- 5-fluoruracil --- pemetrexed --- docking --- 3,4′-bis-guanidino --- 3-amino-4′-guanidino --- diphenyl ether --- phenyl pyridyl ether --- intramolecular hydrogen bond --- cancer cell viability --- HL-60 --- BRAF --- apoptosis --- thieno[2,3-d][1,2,3]triazine --- acetamide --- H1299 --- HER2 --- EGFR --- Bcl-2 inhibitors --- Indole-based analogues --- benzimidazole --- MTT cytotoxic assay --- cell cycle analysis --- DNA fragmentation --- ELISA --- solid/lipid nanoparticles --- phenstatin --- letrozole --- tubulin polymerisation inhibitor --- aromatase inhibitor --- breast cancer --- hybrid molecule --- dual-targeting molecule --- designed multiple ligand --- NaMSA --- cyclophosphamide --- histopathology --- testis --- urinary bladder --- anticancer agents --- enantioselective synthesis --- gastric adenocarcinoma --- tryptophanol --- concentration-guided dosing --- model informed dosing --- physiologically based pharmacokinetics --- sorafenib --- tyrosil-DNA-phosphodiesterase 1 --- adamantane --- resin acid --- TDP1 --- cytotoxic agents --- apoptosis induction --- HT-29 cells --- MDA-MB-231 cells --- mechanism prediction --- STAT inhibitors --- miR-21 --- hydrazide derivatives --- nitrogen scaffolds --- mitoxantrone --- cardiotoxicity --- inflammation --- oxidative stress --- age --- cumulative dose --- Trk --- NTRK --- tissue-agnostic --- larotrectinib --- entrectinib --- Trk fusion --- protein kinase inhibitors --- USFDA --- cancer --- patent review --- generic product --- doxazosin --- MD simulations --- combretastatin A-4 --- cytotoxic activity --- hybrid compounds --- indazole --- mucin --- MUC1 --- MUC16 --- immunotherapy --- cancer vaccine --- CAR (chimeric antigen receptor) --- ADC (antibody-drug conjugate) --- thiourea --- interleukin-6 --- trypan blue assay --- chalcones --- exportin-1 --- covalent binding --- CovDock --- anticancer activity --- xanthone --- in vitro --- in vivo --- isolation --- synthesis --- heterocyclic compound --- benzenesulfonamides --- imidazoles --- alkylated --- colony formation --- tumor spheroids --- HDAC inhibitors --- chalcone --- dual inhibitors --- carvedilol --- kidney --- toxicity --- 7-deaza-4′-thioadenosine derivatives --- multi-kinase inhibitor --- anticancer --- nucleoside --- Imiquimod --- drug efflux --- multidrug resistance --- Toll-Like Receptor --- n/a --- 3,4'-bis-guanidino --- 3-amino-4'-guanidino --- 7-deaza-4'-thioadenosine derivatives

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