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

详细信息    查看全文

• 作者：Euphemia Leung^a ; ^b ; ^{e.leung@auckland.ac.nz" class="auth_mail" title="E-mail the corresponding author} ; Lisa I. Pilkington^a ; ^c ; Michelle van Rensburg^c ; Chae Yeon Jeon^c ; Mirae Song^c ; Homayon J. Arabshahi^c ; Gayan Heruka De Zoysa^c ; Vijayalekshmi Sarojini^c ; William A. Denny^a ; J&oacute ; hannes Reynisson^c ; ^{j.reynisson@auckland.ac.nz" class="auth_mail" title="E-mail the corresponding author} ; David Barker^c ; ^{d.barker@auckland.ac.nz" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Thieno[2 ; 3-b]pyridines ; Thieno[3 ; 2-e]pyridines ; Thieno[2 ; 3-b]quinolones ; Antiproliferative
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2016
• 出版时间：1 March 2016
• 年：2016
• 卷：24
• 期：5
• 页码：1142-1154
• 全文大小：702 K

文摘

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.