Bioorganic & medicinal chemistry

Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors

T Tashima, H Murata, H Kodama

Index: Tashima, Toshihiko; Murata, Hiroaki; Kodama, Hidehiko Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 14 p. 3720 - 3731

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Citation Number: 7

Abstract

Abstract Histone deacetylase (HDAC) inhibitions are known to elicit anticancer effects. We designed and synthesized several HDAC inhibitors. Among these compounds, compound 40 exhibited a more than 10-fold stronger inhibitory activity compared with that of suberoylanilide hydroxamic acid (SAHA) against each human HDAC isozyme in vitro (IC 50 values of 40: HDAC1, 0.0038 μM; HDAC2, 0.0082 μM; HDAC3, 0.015 μM; HDAC8, 0.0060 ...