Design, synthesis and antitumor activity of farnesylthiosalicylamide derivatives
10.11665/j.issn.1000-5048.20150204
- VernacularTitle:新型法尼基硫代水杨酰胺衍生物的设计、合成及抗肿瘤活性
- Author:
Chunfang MAO
1
;
Chenjun XU
;
Xuemin WANG
;
Xianghua LI
;
Wei ZHANG
;
Xinyang WANG
;
Yong LING
Author Information
1. 江苏省南通卫生高等职业技术学校药学系；南通大学药学院
- Publication Type:Journal Article
- Keywords:
farnesylthiosalicylamide;
derivatives synthesis;
antitumor activity;
cell apoptosis
- From:
Journal of China Pharmaceutical University
2015;46(2):162-168
- CountryChina
- Language:Chinese
-
Abstract:
A series of farnesylthiosalicylamide derivatives(9a-9k)were designed and synthesized via condensating the carboxyl of farnesylthiosalicylic acid(FTS)with different amines, and the in vitro biological activity was evaluated. It was observed that eight of them displayed strong antitumor activity against five human cancer cells in vitro. Notably, compound 9k exhibited the most active with the IC50 values of 6. 05-8. 16 μmol/L range against the tested cancer cells, which were superior to those of FTS and even comparable to that of sorafenib in vitro. In addition, compound 9k down-regulated the protein of Bcl-2 and increased the expression levels of Bax and caspase-3 proteins, indicating that compound 9k could induce tumor cell apoptosis.
