Synthesis and cytotoxicity of thieno[2,3-b]quinoline-2-carboxamide and cycloalkyl[b]thieno[3,2-e]pyridine-2-carboxamide derivatives

Publication date: Available online 27 January 2016
Source:Bioorganic & Medicinal Chemistry
Author(s): Euphemia Leung, Lisa I. Pilkington, Michelle van Rensburg, Chae Yeon Jeon, Mirae Song, Homayon J. Arabshahi, Gayan Heruka De Zoysa, Vijayalekshmi Sarojini, William A. Denny, Jóhannes Reynisson, David Barker
Seventy nine derivatives of thieno[2,3–b]quinolines, tetrahydrothieno[2,3-b]quinoline, dihydrocyclopenta[b]thieno[3,2-e]pyridine, cyclohepta[b]thieno[3,2-e]pyridine and hexahydrocycloocta[b]thieno[3,2-e]pyridine were either synthesized or obtained commercially and tested for their antiproliferative activity against HCT116, MDA-MB-468 and MDA-MB-231 human cancer cell lines. The most potent eight compounds were active against all cell lines with IC50 values in the 80-250 nM range. In general hexahydrocycloocta[b]thieno[3,2-e]pyridines were most active with increasing activity observed as larger cycloalkyl rings were fused to the pyridine ring.

Graphical abstract

from #Medicine via ola Kala on Inoreader http://ift.tt/1NFvdNW
via IFTTT