851958-07-1Relevant articles and documents
Discovery of Isoerianin Analogues as Promising Anticancer Agents
Messaoudi, Samir,Hamze, Abdallah,Provot, Olivier,Treguier, Bret,RodrigoDeLosada, Jordi,Bignon, Jerome,Liu, Jian-Miao,Wdzieczak-Bakala, Joanna,Thoret, Sylviane,Dubois, Joelle,Brion, Jean-Daniel,Alami, Mouad
, p. 488 - 497 (2011)
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) invitro, 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.
