title: Design, synthesis and biological evaluation of novel 4-thiazolidinones containing indolin-2-one moiety as potential antitumor agent.
abstract: A series of novel 4-thiazolidinone and indolin-2-one hybrid derivatives 5a-5s and 10a-10s have been designed and synthesized and their cytotoxic activities were evaluated in vitro against three human cancer cell lines including HT-29 (human colon cancer), H460 (human lung cancer), MDA-MB-231 (human breast cancer) by MTT assay. Several potent target compounds (5m, 5p, 5s, 10a, 10c-10g, 10m, 10p) were further evaluated against one cancer cell line SMMC-7721 (human liver cancer) and one normal cell line WI-38 (human fetal lung fibroblasts). Most of the prepared compounds exhibited significant antitumor activities against different human cancer cell lines. Compound 10c (IC(50) = 0.025 μM, 0.075 μM, 0.77 μM, 1.95 μM) was 52, 36, 4.8 and 3.3 times more active than Sunitinib (IC(50) = 1.3 μM, 2.7 μM, 3.7 μM, 6.47 μM) against HT-29, H460, MDA-MB-231 and SMMC-7721 cancer cell line, respectively.
authors.affiliation: Key Laboratory of Original New Drugs Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District 110016, PR China.
authors.forename: Shuobing
authors.initials: S
authors.lastname: Wang
authors.forename: Yanfang
authors.initials: Y
authors.lastname: Zhao
authors.forename: Guogang
authors.initials: G
authors.lastname: Zhang
authors.forename: Yingxiang
authors.initials: Y
authors.lastname: Lv
authors.forename: Ning
authors.initials: N
authors.lastname: Zhang
authors.forename: Ping
authors.initials: P
authors.lastname: Gong
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D003110:Colonic Neoplasms / Q000188:drug therapy / Q000473:pathology; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005260:Female; D005347:Fibroblasts / Q000166:cytology / Q000187:drug effects*; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008113:Liver Neoplasms / Q000188:drug therapy / Q000473:pathology; D008175:Lung Neoplasms / Q000188:drug therapy / Q000473:pathology; D011758:Pyrroles / Q000494:pharmacology; D000077210:Sunitinib; D053778:Thiazolidines / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles; D011758:Pyrroles; D053778:Thiazolidines; C456900:indolin-2-one; D000077210:Sunitinib