- Synthesis and cytotoxic activity of some novel N-pyridinyl-2-(6- phenylimidazo[2,1-b]thiazol-3-yl)acetamide derivatives
-
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 (IC50 = 1.4 μM) compared with sorafenib (IC50 = 5.2 μM), and showed more selectivity against MDA-MB-231 than HepG2 cell line (IC50 = 22.6 μM).
- Ding, Huaiwei,Chen, Zhe,Zhang, Cunlong,Xin, Tian,Wang, Yini,Song, Hongrui,Jiang, Yuyang,Chen, Yuzong,Xu, Yongnan,Tan, Chunyan
-
experimental part
p. 4703 - 4716
(2012/07/01)
-
- Substituted imidazo[2,1-b]thiazoles from 2-aminothiazoles and α-bromo ketones: Efficient preparation and proof of structure
-
The salts formed from α-aminothiazoles and α-bromo ketones (RCOCH2Br) have been basified, and the products converted into amides. Examination of the amides established that they are 2-acylimino-2,3- dihydrothiazoles rather than 2-acylaminothiaz
- Meakins, G. Denis,Musk, Sally R. R.,Robertson, Colin A.,Woodhouse, Lee S.
-
p. 643 - 648
(2007/10/02)
-