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Synthesis and biological evaluation of novel farnesylthiosalicylic acid/salicylic acid hybrids as potential anti-tumor agents |
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| Authors: | Zhi-Qiang Wang Ren-An Chang Hai-Ying Huang Xue-Min Wang Xin-Yang Wang Li Chen Yong Ling |
| Affiliation: | a. Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;b. State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China;c. School of Pharmacy, Nantong University, Nantong 226001, China;d. Department of Hepatobiliary Surgery, Affiliated Hospital, Nantong University, Nantong 226001, China |
| Abstract: | A series of FTS/salicylic acid hybrids was designed and synthesized and their in vitro antitumor activities were evaluated. It was found that the anti-proliferation activities of hybrids were better than that of FTS. Compound 10a displayed the strongest antitumor activities with IC50 values of 5.72-9.76 mmol/L and selectively inhibited tumor cell proliferation. In addition, 10a induced tumor cell apoptosis in a dosedependent manner by up-regulating the expression of Bax and caspase-3 and down-regulating Bcl-2. Our findings suggest that these novel hybrids may hold a great promise as therapeutic agents for the intervention of human cancers. |
| Keywords: | Farnesylthiosalicylic acid Salicylic acid Antitumor activities Cell apoptosis |
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