Discovery of indenopyrazoles as EGFR and VEGFR-2 tyrosine kinase inhibitors by in silico high-throughput screening |
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Authors: | Usui Taikou Ban Hyun Seung Kawada Junpei Hirokawa Takatsugu Nakamura Hiroyuki |
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Affiliation: | Department of Chemistry, Faculty of Science, Gakushuin University, Tokyo 171-8588, Japan. |
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Abstract: | A series of indenopyrazoles 8 and 9 were designed and synthesized as EGFR tyrosine kinase inhibitors by in silico high-throughput screening. Compounds 8b and 8d showed significant inhibition of A431 cell growth (GI50 = 0.062 and 0.057 microM, respectively). Compounds 8b and 9a showed inhibitory activity toward both EGFR and VEGFR-2 (KDR) tyrosine kinases, whereas 8d inhibited VEGFR-2 tyrosine kinase, exclusively. |
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