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Updated: Feb 4, 2026

Efficient iPS Cell Generation from Blood Using Episomes and HDAC Inhibitors
Published on: October 28, 2014
HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors
Rekha Sangwan1, Remya Rajan1, Pintu Kumar Mandal2
1Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram extension, Sitapur Road, P.O. Box 173, Lucknow, 226 031, India.
Abstract:
Even though one is moving towards the success in the discovery of efficient anti-cancer molecules, the drugs used in the treatment of various malignancies are found to possess toxicity and adverse reactivity in the human body that limit their use. The scientists all over the world are engaged in bringing up strategies that aim to develop small molecules that target the abnormal epigenetic factors. The discovery of the role of Histone deacetylases (HDACs) has promised to be a turning point in the treatment of various malignancies. Thus, the invention of potent and safe anticancer therapeutics agents with minimal adverse and side effects are still a major topic of concern and a huge number of research works have been reported in the past few years. This review has been written to discuss on the influence of Histone Deacetylases in cancer malignancies. We have tried to embrace majority of the developments made till date in the field of HDAC and its inhibitors herein. The drugs that are clinically applied, synthesis and SAR study that highlight the chemical groups responsible for evoking the HDAC inhibition and potential of various new classes of HDAC inhibitors (synthetic, hybrid and natural) have also been included.
Insights
Developing safer anti-cancer drugs is crucial. This review explores Histone Deacetylases (HDACs) and their inhibitors, highlighting progress in creating effective cancer therapeutics with fewer side effects.
Area of Science:
- Oncology
- Molecular Biology
- Medicinal Chemistry
Background:
- Current anti-cancer drugs often exhibit toxicity, limiting their clinical application.
- Targeting abnormal epigenetic factors, such as Histone Deacetylases (HDACs), offers a promising strategy for cancer treatment.
- There is a continuous need for potent and safe anticancer therapeutics with minimal adverse effects.
Purpose of the Study:
- To review the role of Histone Deacetylases (HDACs) in cancer malignancies.
- To discuss recent developments in the field of HDACs and their inhibitors.
- To provide an overview of clinically applied drugs, synthesis, SAR studies, and emerging classes of HDAC inhibitors.
Main Methods:
- Literature review focusing on HDACs in cancer.
- Analysis of developments in HDAC inhibitor research.
- Inclusion of data on clinically used drugs, synthesis, structure-activity relationships (SAR), and novel inhibitor classes.
Main Results:
- Histone Deacetylases (HDACs) play a significant role in the development and progression of various cancers.
- Numerous advancements have been made in identifying and developing HDAC inhibitors.
- Various classes of HDAC inhibitors, including synthetic, hybrid, and natural compounds, show potential for cancer therapy.
Conclusions:
- HDACs represent a critical target for novel anti-cancer drug development.
- Continued research into HDAC inhibitors is essential for creating safer and more effective cancer treatments.
- Understanding the SAR of HDAC inhibitors is key to designing potent and selective therapeutic agents.
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