Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2

Szu Lee, Shih Wei Wang, Chen Lin Yu, Huai Ching Tai, Juei Yu Yen, Yu Lien Tuan, Hsueh Hsiao Wang, Yi Ting Liu, Shiou Sheng Chen, Hsueh Yun Lee

研究成果: 雜誌貢獻文章同行評審

摘要

A series of phenylurea hydroxamic acids incorporating pharmacophores of inhibitors of HDAC inhibitors and VEGFR-2 has been designed. Most of the compounds show antiproliferative activity comparable to that of Vorinostat and Sorafenib, and better EPC inhibitory activity. Enzymatic assays and Western blotting results indicated that compound 14 not only inhibits HDAC but also has slight VEGFR-2 inhibitory activity. A docking study revealed that the polar hydroxamic acid retains the interaction with HDAC through a zinc ion and also interacts with some residues of the active site of VEGFR-2. Despite 14 displaying a weaker VEGFR-2 activity, a possible route to develop potent HDAC/VEGFR-2 inhibitors is suggested.

原文英語
文章編號116454
期刊Bioorganic and Medicinal Chemistry
50
DOIs
出版狀態已發佈 - 十一月 15 2021

ASJC Scopus subject areas

  • 生物化學
  • 分子醫學
  • 分子生物學
  • 藥學科學
  • 藥物發現
  • 臨床生物化學
  • 有機化學

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