期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 25, 期 14, 页码 3714-3718出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.05.029
关键词
Carbonic anhydrase; Isatin; 2-Indolinone; Docking
资金
- Istanbul University Scientific Research Projects [ONAP-36808]
Human carbonic anhydrases IX and XII are upregulated in many tumors and form a novel target for new generation anticancer drugs. Here we report the synthesis of novel 2-indolinone derivatives with the sulfonamide group as a zinc binding moiety. Enzyme inhibition assays confirmed that the compounds showed selectivity against hCA IX and XII over the widely distributed off-targets hCA I and II. Molecular modelling studies were performed to suggest modes of binding for these compounds. (C) 2017 Elsevier Ltd. All rights reserved.
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