Synthesis and cytotoxic activity of 3-O-acyl/3-hydrazine /2-bromo/20,29-dibromo betulinic acid derivatives

Abstract A series of 3- O -acyl, 3-hydrazine, 2-bromo, and 20,29-dibromo betulinic acid derivatives ( 1 – 27 ) have been synthesized and screened for in vitro cytotoxic activity on human cancer cell lines MOLT-4, JurkatE6.1, CEM.CM3, BRISTOL8, U937, DU145, PA-1, A549, and L132. A number of compounds have shown ED 50 13 , 19 , 20 , 23 , and 27 were the best derivatives and were selected as lead molecules for further development. The structure–activity relationship has been described.