Harnessing pyrimidine as a building block for histone deacetylase inhibitors

Arch Pharm (Weinheim). 2023 Oct;356(10):e2300208. doi: 10.1002/ardp.202300208. Epub 2023 Jul 18.

Abstract

Histone deacetylase (HDAC) inhibitors are well-established multifaceted bioactive agents against tumors and neurodegenerative disorders. Pyrimidine and its fused and substituted derivatives were employed as a surface recognition moiety of HDAC inhibitors. De facto, the literature was loaded with different success stories of pyrimidine-based HDAC inhibitors that garnered much interest. Provoked by our continuous interest in HDAC inhibitors, we summarized and elaborated on the successful harnessing of the pyrimidine scaffold in this regard. Furthermore, we dissect our perspective that may guide medicinal chemists for an effective future design of more active chemotherapeutic agents with potential clinical applications.

Keywords: HADC inhibitors; antiproliferative; fused pyrimidines; pyrimidines.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Cell Proliferation
  • Histone Deacetylase 1 / pharmacology
  • Histone Deacetylase Inhibitors* / pharmacology
  • Histone Deacetylases / metabolism
  • Histone Deacetylases / pharmacology
  • Pyrimidines / pharmacology
  • Structure-Activity Relationship

Substances

  • Histone Deacetylase Inhibitors
  • Antineoplastic Agents
  • Histone Deacetylases
  • Pyrimidines
  • Histone Deacetylase 1