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Synthesis and in vitro biological evaluation of farnesylthiosalicylic acid derivatives as anti-tumor carcinoma agents
Authors:Yong Linga  You An Xiaob  Guang Tong Chena  Dong Geng Wanga  Yu Qin Lia  Xin Yang Wanga  Heng Zhengc a
Institution:Department of Pharmacy, School of Medical, Nantong University, Nantong 226001, China ; Medicinal College, Anhui College of Traditional Chinese Medicine, Hefei 230031, China ; Department of Bioinformatics, College of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, China
Abstract: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.
Keywords:Synthesis  Farnesylthiosalicylic acid  1  3  4-Thiodiazole  Anti-tumor agents  Cytotoxic activities  Cell apoptosis  
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