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The past decades have seen major developments in the understanding of the cellular and molecular biology of cancer. Significant progress has been achieved regarding long-term survival for the patients of many cancers with the use of tamoxifen for treatment of breast cancer, treatment of chronic myeloid leukaemia with imatinib, and the success of biological drugs. The transition from cytotoxic chemotherapy to targeted cancer drug discovery and development has resulted in an increasing selection of tools available to oncologists. In this Special Issue of Pharmaceuticals, we highlight the opportunities and challenges in the discovery and design of innovative cancer therapies, novel small-molecule cancer drugs and antibody–drug conjugates, with articles covering a variety of anticancer therapies and potential relevant disease states and applications. Significant efforts are being made to develop and improve cancer treatments and to translate basic research findings into clinical use, resulting in improvements in survival rates and quality of life for cancer patients. We demonstrate the possibilities and scope for future research in these areas and also highlight the challenges faced by scientists in the area of anticancer drug development leading to improved targeted treatments and better survival rates for cancer patients.
graphene oxide --- indole --- androgens --- cyclooxygenase-2 --- cyclooxygenase-1 --- heteropolysaccharide --- drug conjugation --- drug delivery --- ellipticine --- chemical linker --- oesophageal cancer --- antiproliferative activity --- topoisomerase II --- ?-lactam --- DSD --- antibody --- topoisomerase inhibitors --- magnetic targeting --- cisplatin resistance --- steroidogenesis --- [18F]FDG PET/CT --- heterocyclic chemistry --- dehydroepiandrosterone --- antimitotic --- 3-vinylazetidin-2-ones --- glioblastoma --- and cancer therapy --- intestinal mucositis --- Combretastatin A-4 --- metabolism --- anti-cancer drugs --- maghemite --- COX-1 inhibitor --- anticancer --- CYP17A1 --- conjugate and hybrid drugs --- inflammation --- snticancer drugs --- P450c17 --- tumorigenesis --- cisplatin --- biomarker profiling --- cancer drug design --- tubulin --- cytochrome P450 --- 5-fluorouracil --- prostate cancer --- abiraterone --- NCI screen --- radiation --- cancer immunotherapy --- microtubule targeted drugs --- cancer --- treatment resistance
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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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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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