Synthesis of N'-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV)

Bioorg Med Chem Lett. 2019 Aug 15;29(16):2369-2374. doi: 10.1016/j.bmcl.2019.06.006.

Maxim V Kozlov ¹, Konstantin A Konduktorov ², Anastasia S Shcherbakova ², Sergey N Kochetkov ²

Affiliations

1 Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Vavilova 32, Moscow 119991, Russia. Electronic address: kozlovmavi@gmail.com.
2 Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Vavilova 32, Moscow 119991, Russia.

PMID: 31201063 DOI: 10.1016/j.bmcl.2019.06.006

Abstract

N'-Propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs), including tubastatin A, vorinostat and belinostat, were synthesized. All prepared compounds inhibited HDAC1/2/3, but not HDAC6, except for one hydrazide analog of HDAC4/5/7 inhibitor that was completely inactive. A novel 4-substituted derivative of N'-propylbenzohydrazide with extremely high anti-HCV activity was discovered.

Keywords

HCV; HDAC; Hydroxamic acid; Inhibitor; N′-Propylhydrazide; Pharmacophore.

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