期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 25, 期 6, 页码 1778-1786出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.01.039
关键词
6-Methoxycarbonyl indolinones; Conformational restriction strategy; Angiokinase inhibitors; Antitumor activity
资金
- Education Department of Liaoning Province [L2015520]
Inhibition of tumor angiogenesis through simultaneously disturbing vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) mediated signaling pathways is a well-established approach in intervention of tumor. A series of 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety were synthesized and evaluated as potent angiokinase inhibitors. Compound 8a demonstrated favorable enzymatic activity against all subtypes of VEGFR and PDGFR. Also, it potently suppressed proliferation of HT-29 cells by inducing apoptosis. Compound 8a has emerged as a promising lead compound for development of angiokinase inhibitors targeting VEGFR and PDGFR. (C) 2017 Elsevier Ltd. All rights reserved.
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