Design, Synthesis, and Evaluation of Benzoheterocyclic-Containing Derivatives as Novel HDAC1 Inhibitors

Abstract In this study, the synthesis and biological evaluation of a variety of benzoheterocyclic-containing benzamide derivatives were described. Some of these compounds were proved to inhibiting the activity of histone deacetylase 1 (HDAC1) with IC 50 values below the micromolar range, retarding p...

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Bibliographic Details
Published in:Pharmaceutical fronts 2022-03, Vol.4 (1), p.e22-e29
Main Authors: Jiao, Min-Ru, Han, Bo, Gu, Xiu, Zhang, Hao, Wang, Ai-Ping, Zhang, Qing-Wei
Format: Article
Language:English
Subjects:
antitumor activity
benzamide derivatives
hdac1 inhibitors
orally active
Original Article
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Summary:Abstract In this study, the synthesis and biological evaluation of a variety of benzoheterocyclic-containing benzamide derivatives were described. Some of these compounds were proved to inhibiting the activity of histone deacetylase 1 (HDAC1) with IC 50 values below the micromolar range, retarding proliferation of several human cancer cells, and surprisingly, not possessing toxicity to human normal cells and hERG K + ion channels. Among those compounds, 3c was the most potent and efficacious derivative. Compound 3c was orally active and displayed excellent in vivo antitumor activity in a HCT-116 xenograft mice model.
ISSN:2628-5088
2628-5096
DOI:10.1055/s-0042-1743487