Structure-activity-relationship studies of conformationally restricted analogs of combretastatin A-4 derived from SU5416.
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.
Pandit
Bulbul
B
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
Sun
Yanjun
Y
Chen
Ping
P
Sackett
Dan L
DL
Hu
Zhigen
Z
Rich
Wendy
W
Li
Chenglong
C
Lewis
Andrew
A
Schaefer
Kevin
K
Li
Pui-Kai
PK
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
D000972:Antineoplastic Agents, Phytogenic; D004273:DNA, Neoplasm; D007211:Indoles; D011758:Pyrroles; D013267:Stilbenes; D014404:Tubulin; C116890:Semaxinib; C058728:fosbretabulin; D011034:Podophyllotoxin