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.

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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