Anticancer Agents : Design, Synthesis and Evaluation
Chen, Qiao-Hong
Anticancer Agents : Design, Synthesis and Evaluation - Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute 2021 - 1 electronic resource (606 p.)
Open Access
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.
Creative Commons
English
books978-3-0365-0141-3 9783036501406 9783036501413
10.3390/books978-3-0365-0141-3 doi
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
Anticancer Agents : Design, Synthesis and Evaluation - Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute 2021 - 1 electronic resource (606 p.)
Open Access
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.
Creative Commons
English
books978-3-0365-0141-3 9783036501406 9783036501413
10.3390/books978-3-0365-0141-3 doi
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