Design, synthesis and biological studies of novel tubulin inhibitors

作者：Sun Yanjun; Pandit Bulbul; Chettiar Somsundaram N; Etter Jonathan P; Lewis Andrew; Johnsamuel Jayasekar; Li Pui Kai^*

来源：Bioorganic & Medicinal Chemistry Letters, 2013, 23(15): 4465-4468.

DOI：10.1016/j.bmcl.2013.04.078

• Anti-microtubule agents
• Tubulin inhibitors

A series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, were synthesized and evaluated. The most potent compound in this series, compound 3, which 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 IC50 values in the low nanomolar range.

• 出版日期2013-8-1