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Acetaminophen. --- Analgesics. --- Analgetics --- Anodynes --- Pain-killing drugs --- Pain relievers --- Painkillers --- Central nervous system depressants --- Acetamidophenol --- Acetaminophenol --- Hydroxyacetanilide --- Hydroxyphenyl acetamide --- Paracetamol --- Acetanilide
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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.
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
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The amide bond represents a privileged motif in chemistry. The recent years have witnessed an explosion of interest in the development of new chemical transformations of amides. These developments cover an impressive range of catalytic N–C bond activation in electrophilic, Lewis acid, radical, and nucleophilic reaction pathways, among other transformations. Equally relevant are structural and theoretical studies that provide the basis for chemoselective manipulation of amidic resonance. This monograph on amide bonds offers a broad survey of recent advances in activation of amides and addresses various approaches in the field.
N-heterocyclic carbene --- non planar amide --- ruthenium (Ru) --- physical organic chemistry --- gemcitabine prodrug --- pyramidal amides --- bridged sultams --- catalysis --- dipeptides --- N-(1-naphthyl)acetamide --- C-N ? bond cleavage --- steric effects --- peptide bond cleavage --- transition-metal-free --- palladium --- N-heterocyclic carbenes (NHCs) --- addition reaction --- C–O activation --- rhodium --- metal complexes --- carbanions --- thioamidation --- amide bond --- intramolecular catalysis --- antiviral activity --- additivity principle --- pre-catalysts --- C–N bond cleavage --- bridged lactams --- C–H acidity --- arynes --- twisted amides --- organic synthesis --- amination --- Suzuki-Miyaura --- tert-butyl --- cyclopentadienyl complexes --- C-S formation --- enzymes --- DFT study --- sulfonamide bond --- N --- HERON reaction --- primaquine --- entropy --- amide activation --- amidation --- synthesis --- amide hydrolysis --- carbonylicity --- amide bond activation --- amide bond resonance --- aminosulfonylation --- molecular dynamics --- model compound --- in situ --- amide --- homogeneous catalysis --- heterocycles --- anomeric effect --- multi-component coupling reaction --- kinetic --- excited state --- C–H bond cleavage --- palladium catalysis --- amides --- thiourea --- formylation --- alkynes --- cis/trans isomerization --- amide C–N bond activation --- intein --- C-H functionalization --- succindiamide --- amide bonds --- crown ether --- aminoacylation --- directing groups --- cytostatic activity --- reaction thermodynamics --- acyl transfer --- transition metals --- N-dimethylformamide --- DMAc --- acylative cross-coupling --- C-H/C-N activation --- nickel catalysis --- antibacterial screening --- sodium --- aryl thioamides --- Winkler-Dunitz parameters --- catalyst --- N-dimethylacetamide --- base-catalyed hydrolysis --- nitrogen heterocycles --- cross-coupling --- insertion --- amidicity --- nitro-aci tautomerism --- activation --- carbonylation --- transamidation --- amine --- distortion --- Pd-catalysis --- rotational barrier energy --- hypersensitivity --- N–C activation --- metabolic stability --- [2+2+2] annulation --- twisted amide --- protease --- cyanation --- amide resonance --- trialkylborane --- catalysts --- biofilm eradication --- pharmacokinetics --- pancreatic cancer cells --- DMF --- aryl esters --- Michael acceptor --- fumardiamide --- water solvation --- ester bond activation --- cyclization --- nuclear magnetic resonance --- secondary amides --- reaction mechanism --- density functional theory --- density-functional theory --- amino acid transporters
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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.
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
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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.
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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