Synthesis and in vitro biological evaluation of farnesylthiosalicylic acid derivatives as anti-tumor carcinoma agents
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- 作者：Yong Ling ; You An Xiao ; Guang Tong Chen ; Dong Geng Wang ; Yu Qin Li ; Xin Yang Wang ; Heng Zheng
- 关键词：Synthesis ; Farnesylthiosalicylic acid ; 1 ; 3 ; 4-Thiodiazole ; Anti-tumor agents ; Cytotoxic activities ; Cell apoptosis
- 刊名：Chinese Chemical Letters
- 出版年：2012
- 出版时间：October, 2012
- 年：2012
- 卷：23
- 期：10
- 页码：1141-1144
- 全文大小：262 K
文摘
Novel farnesylthiosalicylic acid (FTA) derivatives 5a-m with different substituted 1,3,4-thiadiazoles were synthesized. Compounds 5b, 5c, 5e and 5f displayed anti-tumor activities superior to FTA in most cancer cells tested. Furthermore, 5e induced tumor cell apoptosis, which was accompanied by lower Bcl-2 expression, but with higher Bax and caspase 3 expression activities in cancer cells.