title: Structure-activity-relationship studies of conformationally restricted analogs of combretastatin A-4 derived from SU5416.
abstract: A series of combretastatin A-4 analogs derived from the ATP competitive, VEGF receptor tyrosine kinase inhibitor, SU5416 were synthesized. The cytotoxic effects of the analogs were evaluated against PC-3 and MDA-MB-231 cancer cell lines, as well as their abilities to inhibit tubulin polymerization. Results are compared to those of compound 1, our lead compound previously reported.
authors.affiliation: Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
authors.forename: Bulbul
authors.initials: B
authors.lastname: Pandit
authors.forename: Yanjun
authors.initials: Y
authors.lastname: Sun
authors.forename: Ping
authors.initials: P
authors.lastname: Chen
authors.forename: Dan L
authors.initials: DL
authors.lastname: Sackett
authors.forename: Zhigen
authors.initials: Z
authors.lastname: Hu
authors.forename: Wendy
authors.initials: W
authors.lastname: Rich
authors.forename: Chenglong
authors.initials: C
authors.lastname: Li
authors.forename: Andrew
authors.initials: A
authors.lastname: Lewis
authors.forename: Kevin
authors.initials: K
authors.lastname: Schaefer
authors.forename: Pui-Kai
authors.initials: PK
authors.lastname: Li
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid; D004273:DNA, Neoplasm / Q000187:drug effects / Q000235:genetics; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology*; D007536:Isomerism; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation; D011034:Podophyllotoxin / Q000494:pharmacology; D011758:Pyrroles / Q000737:chemistry* / Q000494:pharmacology*; D013267:Stilbenes / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000096:biosynthesis / Q000235:genetics
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004273:DNA, Neoplasm; D007211:Indoles; D011758:Pyrroles; D013267:Stilbenes; D014404:Tubulin; C116890:Semaxinib; C058728:fosbretabulin; D011034:Podophyllotoxin