Novel farnesylthiosalicylic acid （PTA） derivatives 5a-m with different substituted 1,3,4-thiadiazoles were synthesized. Compounds 5b, 5e, 5e and 5f displayed anti-tumor activities superior to FTA in most cancer cell...Novel farnesylthiosalicylic acid （PTA） derivatives 5a-m with different substituted 1,3,4-thiadiazoles were synthesized. Compounds 5b, 5e, 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.展开更多
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.Co...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 10 a displayed the strongest antitumor activities with IC50 values of 5.72-9.76 μmol/L and selectively inhibited tumor cell proliferation.In addition,10 a 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.展开更多
基金support by the Natural Science Foundation of Jiangsu Province in China (NoBK2011389)Applied Research Projects of Nantong City(BK2012085)funded by the Priority Academic Programs Development of Jiangsu Higher Education Institutions(PAPD)
文摘Novel farnesylthiosalicylic acid （PTA） derivatives 5a-m with different substituted 1,3,4-thiadiazoles were synthesized. Compounds 5b, 5e, 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.
基金the Natural Science Foundation of China(No.81302628)Jiangsu Province(No.BK2011389)+1 种基金China Pharmaceutical University for the Open Project Program of State Key Laboratory of Natural Medicines(No.SKLNMKF201415) for the financial supporta project funded by the Priority Academic Programs Development(PAPD) of Jiangsu Higher Education Institutions
文摘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 10 a displayed the strongest antitumor activities with IC50 values of 5.72-9.76 μmol/L and selectively inhibited tumor cell proliferation.In addition,10 a 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.
