Synthesis and evaluation of antitumoral activity of ester and amide derivatives of 2-arylamino-6- trifluoromethyl-3-pyridinecarboxylic acids

The synthesis and antitumoral activity of ester and amide derivatives of 2-arylamino-6-trifluoromethyl-3-pyridinecarboxylic acids 8–58 is described. Trifluoromethylpyridine derivatives 8–58 were evaluated for their anticancer activity toward human tumoral cell lines by the National Cancer Institute (NCI). Most of them possess encouraging anticancer activity, having GI50 values in the low micromolar to nanomolar concentration range. The 3,4,5-trimethoxyphenylamide 44 was the most active, and it is now under review by NCI Biological Evaluation Committee for possible further studies.