title: Conformationally restricted analogs of Combretastatin A-4 derived from SU5416.
abstract: A series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, was synthesized and evaluated. The most potent compound in this series, compound 7, 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 IC(50) values in low to subnanomolar range.
authors.affiliation: Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA. li.27@osu.edu
authors.forename: Pui-Kai
authors.initials: PK
authors.lastname: Li
authors.forename: Zili
authors.initials: Z
authors.lastname: Xiao
authors.forename: Zhigen
authors.initials: Z
authors.lastname: Hu
authors.forename: Bulbul
authors.initials: B
authors.lastname: Pandit
authors.forename: Yanjun
authors.initials: Y
authors.lastname: Sun
authors.forename: Dan L
authors.initials: DL
authors.lastname: Sackett
authors.forename: Karl
authors.initials: K
authors.lastname: Werbovetz
authors.forename: Andrew
authors.initials: A
authors.lastname: Lewis
authors.forename: Jayasekar
authors.initials: J
authors.lastname: Johnsamuel
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D001921:Brain / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D002455:Cell Division / Q000187:drug effects; D007211:Indoles / Q000737:chemistry*; D008958:Models, Molecular; D008968:Molecular Conformation; D011758:Pyrroles / Q000737:chemistry*; D013267:Stilbenes / Q000737:chemistry*; D013552:Swine; D014404:Tubulin / Q000187:drug effects / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles; D011758:Pyrroles; D013267:Stilbenes; D014404:Tubulin; C116890:Semaxinib; C058728:fosbretabulin