Conformationally restricted analogs of Combretastatin A-4 derived from SU5416.


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.

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@article{Li2005ConformationallyRA, title={Conformationally restricted analogs of Combretastatin A-4 derived from SU5416.}, author={Pui-kai Li and Zili Xiao and Zhigen Hu and Bulbul Pandit and Yanjun Sun and Dan L. Sackett and Karl A. Werbovetz and Andrew S . Lewis and Jayasekar Johnsamuel}, journal={Bioorganic & medicinal chemistry letters}, year={2005}, volume={15 24}, pages={5382-5} }