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• W2213661638 abstract "A series of novel pyrazole-nitroimidazole derivatives had been arranged and evaluated for their EGFR/HER-2 tyrosine kinase inhibitory activity as well as their antiproliferative properties on four kinds of cancer cell lines (MCF-7, Hela, HepG2, B16-F10). The bioassay results showed most of the designed compounds exhibited potential antiproliferation activity, with the IC50 values ranging from 0.13 μM to 128.06 μM in four tumor cell lines. Among them, compound 5c exhibited remarkable inhibitory activity against EGFR/HER-2 tyrosine kinase with IC50 value of 0.26 μM/0.51 μM, respectively, comparable to the positive control erlotinib (IC50 = 0.41 μM for HER-2 and IC50 = 0.20 μM for EGFR) and lapatinib (IC50 = 0.54 μM for HER-2 and IC50 = 0.28 μM for EGFR). Molecular modeling simulation studies were performed in order to predict the biological activity of the proposed compounds and activity relationship (SAR) of these pyrazole-nitroimidazole derivatives." @default.
• W2213661638 created "2016-06-24" @default.
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• W2213661638 date "2016-01-01" @default.
• W2213661638 modified "2023-10-18" @default.
• W2213661638 title "Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors" @default.
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• W2213661638 doi "https://doi.org/10.1016/j.bmcl.2015.11.040" @default.
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