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Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors

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 Mann... Full description

Journal Title: Bioorganic & Medicinal Chemistry 15 March 2017, Vol.25(6), pp.1778-1786
Main Author: Qin, Mingze
Other Authors: Yan, Shuang , Wang, Lei , Zhang, Haotian , Tian, Ye , Zhao, Yanfang , Gong, Ping
Format: Electronic Article Electronic Article
Language: English
Subjects:
ID: ISSN: 0968-0896 ; E-ISSN: 1464-3391 ; DOI: 10.1016/j.bmc.2017.01.039
Link: https://www.sciencedirect.com/science/article/pii/S0968089616311130
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recordid: elsevier_sdoi_10_1016_j_bmc_2017_01_039
title: Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors
format: Article
creator:
  • Qin, Mingze
  • Yan, Shuang
  • Wang, Lei
  • Zhang, Haotian
  • Tian, Ye
  • Zhao, Yanfang
  • Gong, Ping
subjects:
  • 6-Methoxycarbonyl Indolinones
  • Conformational Restriction Strategy
  • Angiokinase Inhibitors
  • Antitumor Activity
  • Medicine
  • Chemistry
  • Anatomy & Physiology
ispartof: Bioorganic & Medicinal Chemistry, 15 March 2017, Vol.25(6), pp.1778-1786
description: 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 demonstrated favorable enzymatic activity against all subtypes of VEGFR and PDGFR. Also, it potently suppressed proliferation of HT-29 cells by inducing apoptosis. Compound has emerged as a promising lead compound for development of angiokinase inhibitors targeting VEGFR and PDGFR.
language: eng
source:
identifier: ISSN: 0968-0896 ; E-ISSN: 1464-3391 ; DOI: 10.1016/j.bmc.2017.01.039
fulltext: fulltext
issn:
  • 0968-0896
  • 09680896
  • 1464-3391
  • 14643391
url: Link


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descriptionInhibition 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 demonstrated favorable enzymatic activity against all subtypes of VEGFR and PDGFR. Also, it potently suppressed proliferation of HT-29 cells by inducing apoptosis. Compound has emerged as a promising lead compound for development of angiokinase inhibitors targeting VEGFR and PDGFR.
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