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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Review Article

Heterocyclic Moieties as HDAC Inhibitors: Role in Cancer Therapeutics

Author(s): Sharba Tasneem, Mohammad Mumtaz Alam*, Mohammad Amir, Mymoona Akhter, Suhel Parvez, Garima Verma, Lalit Mohan Nainwal, Ashif Equbal, Tarique Anwer and Mohammad Shaquiquzzaman*

Volume 22, Issue 12, 2022

Published on: 07 February, 2022

Page: [1648 - 1706] Pages: 59

DOI: 10.2174/1389557519666211221144013

Price: $65


‘Epigenetic’ regulation of genes via post-translational modulation of proteins is a wellexplored approach for disease therapies, particularly cancer chemotherapeutics. Histone deacetylases (HDACs) are one of the important epigenetic targets and are mainly responsible for balancing the acetylation/deacetylation of lysine amino acids on histone/nonhistone proteins along with histone acetyltransferase (HAT). HDAC inhibitors (HDACIs) have become important biologically active compounds for the treatment of cancers due to cell cycle arrest, differentiation, and apoptosis in tumor cells, thus leading to anticancer activity. Out of the four classes of HDAC, i.e., Class I, II, III, and IV, HDACIs act on Class IV (Zinc dependent HDAC), and various FDA-approved drugs belong to this category. The required canonical pharmacophore model (zinc-binding group, surface recognition cap, and appropriate linker) supported by HDACIs, various heterocyclic moieties containing compounds exhibiting HDAC inhibitory activity, and structure-activity relationship of different synthetic derivatives reported during the last twelve years have been summarized in this review.

Keywords: Histone deacetylase, histone deacetylase inhibitors, tubulin, cancer, structure-activity relationship, heterocyclic moieties.

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Definition of cancer - NCI Dictionary of Cancer Terms - National Cancer Institute. Available from:
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