Synthesis and In Vitro Studies of O-Alkylaminoethylated Derivatives of 3E-Hydroximinocholestene as Potent and Selective Antileukemic Agents

Abstract

New O-alkylaminoethylated derivatives of 3-hydroximinocholestene were synthesised and studied for in vitro cytotoxic effects. The obtained oily oxime ethers were solidified by preparing their oxalate salts. The steroidal compounds were screened against 60 human cancer cell lines at 10 μM. The study indicated that the compounds display selective cytotoxicity against leukemia cell lines. Dimethylamine (7a) and pyrrolidine (7d) derived O-alkylated steroidal oxalates displayed percent growth inhibition of 73.36%and 69.97 %, respectively, against CCRF-CEM leukemia cancer cell line. Partition coefficient values of the new steroids were also estimated to study the correlation of lipophilicity with the biological activity. The overall percentage growth inhibition of leukemia cell lines was 42% and 41% when treated with compounds 7a and 7d, respectively. Results obtained in the present study would help developing potent cytotoxic compounds with specificity toward leukemia cancer.