Structure-activity-relationship studies of conformationally restricted analogs of combretastatin A-4 derived from SU5416.
Pandit B., Sun Y., Chen P., Sackett DL., Hu Z., Rich W., Li C., Lewis A., Schaefer K., Li P-K.
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.