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An Overview of HDAC Inhibitors and their Synthetic Routes

Xiaopeng Peng1,2, Guochao Liao3, Pinghua Sun4

  • 1School of Pharmaceutical Sciences, Guangdong Provincial Key Laboratory of New Drug Screening, Southern Medical University, Guangzhou 510515, China.

Current Topics in Medicinal Chemistry
|March 5, 2019
PubMed

Insights

Histone deacetylases (HDACs) are crucial in cancer development. This review summarizes recent histone deacetylase inhibitors (HDACi) and discusses future directions for novel anti-cancer therapeutics.

Area of Science:

  • Oncology
  • Epigenetics
  • Biochemistry

Background:

  • Epigenetic modifications, including histone acetylation, are vital in cancer initiation, progression, and metastasis.
  • Histone deacetylases (HDACs) regulate critical cellular functions like DNA repair and cell cycle control, and their dysregulation can activate oncogenes.
  • Histone deacetylase inhibitors (HDACi) have emerged as promising anti-cancer therapeutics due to the critical role of HDACs in tumorigenesis.

Purpose of the Study:

  • To provide a comprehensive summary of recent advancements in histone deacetylase inhibitors (HDACi).
  • To review the synthetic routes employed in the development of novel HDAC inhibitors.
  • To discuss future perspectives and potential directions for the development of new anti-cancer HDACi.

Main Methods:

  • Literature review of recent studies on HDAC inhibitors.
  • Analysis of synthetic pathways for HDAC inhibitor development.
  • Discussion of current research trends and future prospects in HDAC inhibitor therapy.

Main Results:

  • Significant progress has been made in understanding the role of HDACs in cancer.
  • Numerous HDAC inhibitors have been developed, with ongoing research into their synthesis and efficacy.
  • The therapeutic potential of HDACi in various cancers is increasingly recognized.

Conclusions:

  • HDACs are validated targets for cancer therapy, with HDACi showing considerable promise.
  • Continued research into novel HDAC inhibitors and their synthetic routes is essential for advancing cancer treatment.
  • Future development should focus on optimizing HDACi for improved efficacy and targeted delivery in anti-cancer strategies.
Keywords:
CancerDNAEpigeneticsHDACInhibitorsSynthetic routes.

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