Hydroxamic acids as histone deacetylase inhibitors

Florian Thaler, Vaishali M. Patil, Satya P. Gupta

Research output: Chapter in Book/Report/Conference proceedingChapter

Abstract

HDAC inhibition has been, for over a decade (and continues to remain), a highly competitive area. Hydroxamic acids represent the largest class of HDAC inhibitors. One product, SAHA is already approved and more than ten different chemical entities are in various clinical stages. A detailed discussion about compounds from various classes like phenyloxopropenyl, amidopropenyl analogues, spiropiperidines, biphenyl/arylamide/styrenyl, tetrahydroisoquinoline-based hydroxamic acid derivatives and N-hydroxyphenylacrylamide derivatives has been included along with the computational studies. It also covers brief details about the HDAC imaging agents. These successes as well as the enormous amount of experiences gained in preclinical and clinical studies may be useful-beyond the HDAC field-to future drug discovery programmes studying hydroxamic acid derivatives.

Original languageEnglish
Title of host publicationHydroxamic Acids: A Unique Family of Chemicals with Multiple Biological Activities
PublisherSpringer-Verlag Berlin Heidelberg
Pages99-151
Number of pages53
ISBN (Print)9783642381119, 3642381103, 9783642381102
DOIs
Publication statusPublished - Jul 1 2013

Keywords

  • Chromatin
  • HDAC inhibitors
  • Histone deacetylases
  • Isoform selectivity
  • Nucleosome
  • Oral bioavailability

ASJC Scopus subject areas

  • Chemistry(all)

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  • Cite this

    Thaler, F., Patil, V. M., & Gupta, S. P. (2013). Hydroxamic acids as histone deacetylase inhibitors. In Hydroxamic Acids: A Unique Family of Chemicals with Multiple Biological Activities (pp. 99-151). Springer-Verlag Berlin Heidelberg. https://doi.org/10.1007/978-3-642-38111-9_5