Design, synthesis, biological evaluation and molecular docking studies of novel benzofuran–pyrazole derivatives as anticancer agents
作者： Somaia S. Abd El-Karim , Manal M. Anwar , Neama A. Mohamed , Tamer Nasr , Samia A. Elseginy
DOI: 10.1016/J.BIOORG.2015.08.006
关键词:
摘要: This study deals with design and synthesis of novel benzofuran-pyrazole hybrids as anticancer agents. Eight compounds were chosen by National Cancer Institute (NCI), USA to evaluate their in vitro antiproliferative activity at 10(-5)M full NCI 60 cell panel. The preliminary screening the tested showed promising broad-spectrum activity. Compound 4c was further assayed for five dose molar ranges panel exhibited remarkable growth inhibitory pattern against Leukemia CCRF-CEM, MOLT-4, Lung HOP-92, Colon HCC-2998, CNS SNB-75, Melanoma SK-MEL-2, Ovarian IGROV1, Renal 786-0, RXF 393, Breast HS 578T T-47D (GI50: 1.00-2.71μM). Moreover, enzyme assays carried out investigate possible mechanism action compound 4c. results revealed that has good c-Src 10μM. In addition, molecular docking studies could bind ATP Src pocket sites. Fulfilling Lipinskiis rule addition its ADME profile biological results, all strongly suggest is a kinase inhibitor.
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