Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agents.

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Lv PC, Li HQ, Sun J, Zhou Y, Zhu HL

Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agents.

Bioorg Med Chem. 2010 Jul 1;18(13):4606-14. doi: 10.1016/j.bmc.2010.05.034. Epub 2010 May 20.

PubMed ID
20627597 [ View in PubMed
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Abstract

Two series of pyrazole derivatives designing for potential EGFR kinase inhibitors have been discovered. Some of them exhibited significant EGFR inhibitory activity. Compound 3-(3,4-dimethylphenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioami de (C5) displayed the most potent EGFR inhibitory activity with IC(5)(0) of 0.07 muM, which was comparable to the positive control erlotinib. Docking simulation was performed to position compound C5 into the EGFR active site to determine the probable binding model. Antiproliferative assay results indicating that some of the pyrazole derivatives own high antiproliferative activity against MCF-7. Compound C5 showed significant antiproliferative activity against MCF-7 with IC(5)(0) of 0.08 muM. Therefore, compound C5 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