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


  • 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)<1 microg/mL against the cancer cell lines tested and have shown better cytotoxicity than betulinic acid. Compounds 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.

published proceedings

  • Bioorg Med Chem Lett

altmetric score

  • 3

author list (cited authors)

  • Mukherjee, R., Jaggi, M., Siddiqui, M., Srivastava, S. K., Rajendran, P., Vardhan, A., & Burman, A. C.

citation count

  • 29

complete list of authors

  • Mukherjee, Rama||Jaggi, Manu||Siddiqui, Mohammad JA||Srivastava, Sanjay K||Rajendran, Praveen||Vardhan, Anand||Burman, Anand C

publication date

  • August 2004