title: Design, synthesis and biological studies of novel tubulin inhibitors.
abstract: A series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, were synthesized and evaluated. The most potent compound in this series, compound 3, which structurally resembles the potent anti-microtubule agent combretastatin A-4, inhibited tubulin polymerization and showed potent growth inhibitory activities on both prostate and breast cancer lines with IC50 values in the low nanomolar range.
authors.affiliation: Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 338 Parks Hall, 500 West 12th Avenue, Columbus, OH 43210-1291, United States.
authors.forename: Yanjun
authors.initials: Y
authors.lastname: Sun
authors.forename: Bulbul
authors.initials: B
authors.lastname: Pandit
authors.forename: Somsundaram N
authors.initials: SN
authors.lastname: Chettiar
authors.forename: Jonathan P
authors.initials: JP
authors.lastname: Etter
authors.forename: Andrew
authors.initials: A
authors.lastname: Lewis
authors.forename: Jayasekar
authors.initials: J
authors.lastname: Johnsamuel
authors.forename: Pui-Kai
authors.initials: PK
authors.lastname: Li
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001632:Bibenzyls / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D015195:Drug Design; D006801:Humans; D058105:Polymerization / Q000187:drug effects; D014404:Tubulin / Q000737:chemistry / Q000378:metabolism*; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D001632:Bibenzyls; D014404:Tubulin; D050257:Tubulin Modulators; C040105:combretastatin