Discovery of Isoerianin Analogues as Promising Anticancer Agents
Citations Over TimeTop 1% of 2011 papers
Abstract
The cytotoxic activity of a series of 23 new isoerianin derivatives with modifications on both the A and B rings was studied. Several compounds exhibited excellent antiproliferative activity at nanomolar concentrations against a panel of human cancer cell lines. The most cytotoxic compound, isoerianin (3), strongly inhibits tubulin polymerization in the micromolar range. Moreover, isoerianin leads to G2/M phase cell-cycle arrest in H1299 and K562 cancer cells, and strongly induces apoptosis. Isoerianin also disrupts the vessel-like structures formed by human umbilical vein endothelial cells (HUVECs) in vitro, suggesting that this compound may act as a vascular disrupting agent. It clearly appears that in this compound series, the 1,1-ethane bridge encountered in isoerianin derivatives can replace the 1,2-ethane bridge of natural erianin with no loss of activity. This reinforces the bioisosteric replacement approach in the combretastatin series previously reported by our research group.
Related Papers
- → Combretastatin-like chalcones as inhibitors of microtubule polymerization. Part 1: Synthesis and biological evaluation of antivascular activity(2009)188 cited
- → The interaction with tubulin of a series of stilbenes based on combretastatin A-4(1995)174 cited
- → A 2-step synthesis of Combretastatin A-4 and derivatives as potent tubulin assembly inhibitors(2020)14 cited
- Effects of buthionine sulfoxine on the redox state of human umbilical vein endothelial cells cultured with K562 cells conditioned media(2005)
- Enhancement Effect of K562 Cells Supernatant on Proliferation of Human Umbilical Vein Endothelial Cells(2009)