Design, synthesis and biological evaluation of thiazolidinone derivatives as potential EGFR and HER-2 kinase inhibitors.

Article Details

Citation

Lv PC, Zhou CF, Chen J, Liu PG, Wang KR, Mao WJ, Li HQ, Yang Y, Xiong J, Zhu HL

Design, synthesis and biological evaluation of thiazolidinone derivatives as potential EGFR and HER-2 kinase inhibitors.

Bioorg Med Chem. 2010 Jan 1;18(1):314-9. doi: 10.1016/j.bmc.2009.10.051. Epub 2009 Oct 30.

PubMed ID
19914835 [ View in PubMed
]
Abstract

Two series of thiazolidinone derivatives designing for potential EGFR and HER-2 kinase inhibitors have been discovered. Some of them exhibited significant EGFR and HER-2 inhibitory activity. Compound 2-(2-(5-bromo-2-hydroxybenzylidene)hydrazinyl)thiazol-4(5H)-one (12) displayed the most potent inhibitory activity (IC(50)=0.09 microM for EGFR and IC(50)=0.42 microM for HER-2), comparable to the positive control erlotinib. Docking simulation was performed to position compound 12 into the EGFR active site to determine the probable binding model. Antiproliferative assay results indicating that some of the thiazolidinone derivatives own high antiproliferative activity against MCF-7. Compound 12 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
ErlotinibEpidermal growth factor receptorIC 50 (nM)30N/AN/ADetails