title: 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.affiliation: Divisions of Experimental Oncology, Dabur Research Foundation, 22, Site IV, Sahibabad, Ghaziabad 201 010, UP, India.
authors.forename: Rama
authors.initials: R
authors.lastname: Mukherjee
authors.forename: Manu
authors.initials: M
authors.lastname: Jaggi
authors.forename: Praveen
authors.initials: P
authors.lastname: Rajendran
authors.forename: Mohammad J A
authors.initials: MJ
authors.lastname: Siddiqui
authors.forename: Sanjay K
authors.initials: SK
authors.lastname: Srivastava
authors.forename: Anand
authors.initials: A
authors.lastname: Vardhan
authors.forename: Anand C
authors.initials: AC
authors.lastname: Burman
mesh_terms: D020533:Angiogenesis Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D053978:Pentacyclic Triterpenes; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology*; D000094062:Betulinic Acid
chemical_list: D020533:Angiogenesis Inhibitors; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; D000094062:Betulinic Acid