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  • Title: Discovery of isoerianin analogues as promising anticancer agents.
    Author: Messaoudi S, Hamze A, Provot O, Tréguier B, Rodrigo De Losada J, Bignon J, Liu JM, Wdzieczak-Bakala J, Thoret S, Dubois J, Brion JD, Alami M.
    Journal: ChemMedChem; 2011 Mar 07; 6(3):488-97. PubMed ID: 21360820.
    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.
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