Betulinic acid and its derivatives as anti-angiogenic agents.

abstract

• Betulinic acid (1) significantly caused cytotoxicity to endothelial cell line ECV304 (IC(50) 1.26+/-0.44 microg/mL) in a 5-day MTT assay. Novel and more potent derivatives of betulinic acid (2, 4, 6-8) have been synthesized with IC(50) less than 0.4 microg/mL. The endothelial cell specificity against human tumor cell lines DU145, L132, A549, and PA-1 were determined. Further betulinic acid (1) inhibited TLS formation of ECV304 cells on Matrigel(TM) by 5.5% while its derivatives caused an inhibition of 13.1-49.2%.

authors

• Rajendran, Praveen

published proceedings

• Bioorg Med Chem Lett

author list (cited authors)

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

citation count

• 57

complete list of authors

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

publication date

• May 2004

publisher

• Elsevier  Publisher

published in

• Bioorganic and Medicinal Chemistry Letters  Journal

keywords

• Angiogenesis Inhibitors
• Betulinic Acid
• Cell Line, Tumor
• Humans
• Pentacyclic Triterpenes
• Structure-Activity Relationship
• Triterpenes

PubMed Central ID

• 15081004

Digital Object Identifier (DOI)

• 10.1016/j.bmcl.2004.02.044

start page

• 2181

end page

• 2184

volume

• 14

issue

• 9

URL

• http://dx.doi.org/10.1016/j.bmcl.2004.02.044