Histone Deacetylase Inhibitors: A Brief Overview Of Their Role And Medicinal Chemistry

Abstract

Histone deacetylases (HDACs) comprise a family of proteins that impact critical cellular processes through regulation of chromatin remodeling and gene transcription. HDACs have emerged as attractive targets for the development of new anticancer agents and a number of structurally diverse inhibitors of HDAC from natural or synthetic origin have been described in the literature. This chapter focuses on those having reached clinical phases. For each, synthesis pathway, in vitro properties and short clinical profiles are presented. Recent developments in medicinal chemistry of HDAC inhibition are also reported. Keywords: anticancer-agents; chromatin; HDAC; JNJ-26481585; histone deacetylase; hydroxamic acid; R306465