title: Synthesis and cytotoxic activity of some novel N-pyridinyl-2-(6-phenylimidazo[2,1-b]thiazol-3-yl)acetamide derivatives.
abstract: A series of novel compounds bearing imidazo[2,1-b]thiazole scaffolds were designed and synthesized based on the optimization of the virtual screening hit compound N-(6-morpholinopyridin-3-yl)-2-(6-phenylimidazo[2,1-b]thiazol-3-yl)acetamide (5a), and tested for their cytotoxicity against human cancer cell lines, including HepG2 and MDA-MB-231. The results indicated that the compound 2-(6-(4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl)-N-(6-(4-(4-methoxybenzyl)piperazin-1-yl)pyridin-3-yl)acetamide (5l), with slightly higher inhibition on VEGFR2 than 5a (5.72% and 3.76% inhibitory rate at 20 μM, respectively), was a potential inhibitor against MDA-MB-231 (IC(50) = 1.4 μM) compared with sorafenib (IC(50) = 5.2 μM), and showed more selectivity against MDA-MB-231 than HepG2 cell line (IC(50) = 22.6 μM).
authors.affiliation: School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China. dinghuaiwei627@163.com
authors.forename: Huaiwei
authors.initials: H
authors.lastname: Ding
authors.forename: Zhe
authors.initials: Z
authors.lastname: Chen
authors.forename: Cunlong
authors.initials: C
authors.lastname: Zhang
authors.forename: Tian
authors.initials: T
authors.lastname: Xin
authors.forename: Yini
authors.initials: Y
authors.lastname: Wang
authors.forename: Hongrui
authors.initials: H
authors.lastname: Song
authors.forename: Yuyang
authors.initials: Y
authors.lastname: Jiang
authors.forename: Yuzong
authors.initials: Y
authors.lastname: Chen
authors.forename: Yongnan
authors.initials: Y
authors.lastname: Xu
authors.forename: Chunyan
authors.initials: C
authors.lastname: Tan
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D013844:Thiazoles / Q000138:chemical synthesis* / Q000633:toxicity*; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors
chemical_list: D000081:Acetamides; D000970:Antineoplastic Agents; C574115:N-pyridinyl-2-(6-phenylimidazo(2,1-b)thiazol-3-yl)acetamide; D047428:Protein Kinase Inhibitors; D013844:Thiazoles; D040301:Vascular Endothelial Growth Factor Receptor-2