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)<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.

authors

• Rajendran, Praveen

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

publisher

• Elsevier  Publisher

published in

• Bioorganic and Medicinal Chemistry Letters  Journal

keywords

• Antineoplastic Agents
• Betulinic Acid
• Cell Line
• Cell Line, Tumor
• Cell Survival
• Humans
• Hydrazines
• Jurkat Cells
• Models, Molecular
• Molecular Conformation
• Pentacyclic Triterpenes
• Triterpenes

PubMed Central ID

• 15225732

Digital Object Identifier (DOI)

• 10.1016/j.bmcl.2004.05.034

start page

• 4087

end page

• 4091

volume

• 14

issue

• 15

URL

• http://dx.doi.org/10.1016/j.bmcl.2004.05.034