Design, Synthesis, and Biological Evaluation of Dual c-Met/HDAC Inhibitors Bearing 2-Aminopyrimidine Scaffold

Design, Synthesis, and Biological Evaluation of Dual c-Met/HDAC Inhibitors Bearing 2-Aminopyrimidine Scaffold

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A series of c-Met/histone deacetylase (HDAC) bifunctional inhibitors was designed and synthesized by merging pharmacophores of c-Met and HDAC inhibitors. Among them, the most potent compound, 2o, inhibited c-Met kinase and HDACs, with IC50 values of 9.0 and 31.6 nM, respectively, and showed efficien...

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Bibliographic Details
Main Authors: Qingwei Zhang, Guili Xu, Ya Bao, Minru Jiao, Jianqi Li
Format: Article
Language:English
Published: Georg Thieme Verlag KG 2020-09-01
Series:Pharmaceutical Fronts
Subjects:
c-met/hdac inhibitor
dual inhibitor
hybrid
antitumor drugs
multipharmacology
Online Access:http://www.thieme-connect.de/DOI/DOI?10.1055/s-0040-1722543

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