摘要
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.
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.
基金
the Natural Science Foundation of China(No.81302628)
Jiangsu Province(No.BK2011389)
China Pharmaceutical University for the Open Project Program of State Key Laboratory of Natural Medicines(No.SKLNMKF201415) for the financial support
a project funded by the Priority Academic Programs Development(PAPD) of Jiangsu Higher Education Institutions
