Synthesis and biological evaluation of novel farnesylthiosalicylic acid/salicylic acid hybrids as potential anti-tumor agents

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 μmol/L and selectively inhibited tumor cell proliferation. In addition, 10a induced tumor cell apoptosis in a dose-dependent 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. Compound 10a exhibited the strongest anti-tumor activities, and selectively inhibited tumor cell proliferation which might be mediated by apoptosis via the down-regulation of Bcl-2 and up-regulation of Bax and caspase-3.Figure optionsDownload as PowerPoint slide