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Histone Deacetylase 2 (HDAC2) Inhibitors Containing Boron
Author(s) -
Kavianpour Poya,
Gemmell Madeleine C. M.,
Kahlert Jan U.,
Rendina Louis M.
Publication year - 2020
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.202000131
Subject(s) - vorinostat , histone deacetylase , chemistry , histone deacetylase inhibitor , histone deacetylase 2 , enzyme , hdac10 , histone , biochemistry , gene
Histone deacetylase enzymes (HDACs) are responsible for the global silencing of tumour‐suppressor genes. Treatment with a histone deacetylase inhibitor (HDACi) can reverse this process and restore normal cell function. Herein, we report a small series of boron‐based (boronic acid, boronate ester and closo‐ 1,2‐carborane) HDAC2 inhibitors with IC 50 values in the nanomolar range. The boronate ester 4 b was the most potent compound assessed in this study (IC 50 =40.6±1.5 nM), followed closely by the 1,2‐ closo ‐carborane (IC 50 =42.9±1.5 nM). Compound 4 b exceeds the potency of the related gold‐standard HDAC pan‐inhibitor vorinostat ( 1 ) toward this particular HDAC isoform.