Anticancer Agents

Design, Synthesis and Evaluation

Edited by
March 2021
606 pages
  • ISBN978-3-0365-0140-6 (Hardback)
  • ISBN978-3-0365-0141-3 (PDF)

This book is a reprint of the Special Issue Anticancer Agents: Design, Synthesis and Evaluation that was published in

Chemistry & Materials Science
Medicine & Pharmacology
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.
  • Hardback
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© 2022 by the authors; CC BY-NC-ND license
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; HeLa; 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; anticancer activity; breast cancer; benzofuran–pyrazole; nanoparticles; cytotoxic activity; apoptosis; PARP-1 inhibition; 3,6-dibromocarbazole; 5-bromoindole; carbazole; actin; breast cancer; migration; Thienopyrimidine; Pyrazole; PI3Kα inhibitor; quinazolin-4(3H)-one; quinazolin-4(3H)-thione; Schiff base; antiproliferative activity; antioxidant activity; DFT study; ortho-quinones; antitumor activity; beta-lapachone; tanshione IIA; PI3Ks; PI3Kδ inhibitors; 2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide; anticancer; anticancer agents; protein–protein interactions; virtual screening; mimetics; drug discovery; bivalency; polyvalency; antitumor; apoptosis; cell cycle; ovarian cancer; P-MAPA; IL-12; TLR signaling; inflammation; chemoresistance; 4-(pyridin-4-yloxy)benzamide; 1,2,3-triazole; c-Met; inhibitor; natural product; anticancer agent; synthesis; zampanolide; Talazoparib; PARP inhibitor; prodrug; o-nitro-benzyl; photoactivatable protecting groups; salinomycin; anticancer activity; overcoming drug resistance; tumor specificity; synergy; 5-fluorouracil; gemcitabine; amides/esters; ovarian cancer; colchicine analogs; thiocolchicine; colchiceine; antimitotic agents; antiproliferative activity; hydrates; dihydropyranoindole; anticancer; HDAC inhibitors; neuroblastoma; breast cancer; 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; anticancer agents; colchicine amide; colchicine sulfonamide; tubulin inhibitors; docking studies; crystal structure; PROTACs; anticancer activity; protein degradation; IGF-1R; Src; protein kinase; phenylpyrazolopyrimidine; antiproliferative activity; enzyme inhibition; molecular simulation; androgen receptor; prostate cancer; enzalutamide; apalutamide; darolutamide; triple-negative breast cancer; cytotoxicity; chrysin analogues; flavonoid; anticancer compounds