Synthesis of 7200 small molecules based on a substructural analysis of the histone deacetylase inhibitors trichostatin and trapoxin

Scott M. Sternson, Jason C. Wong, Christina M. Grozinger, Stuart L. Schreiber

Research output: Contribution to journalArticlepeer-review

147 Scopus citations

Abstract

(Formula Presented) Seventy-two hundred potential inhibitors of the histone deacetylase (HDAC) enzyme family, based on a 1,3-dioxane diversity structure, were synthesized on polystyrene macrobeads. The compounds were arrayed for biological assays in a "one bead-one stock solution" format. Metal-chelating functional groups were used to direct the 1,3-dioxanes to HDAC enzymes, which are zinc hydrolases. Representative structures from this library were tested for inhibitory activity and the 1,3-dioxane structure was shown to be compatible with HDAC inhibition.

Original languageEnglish (US)
Pages (from-to)4239-4242
Number of pages4
JournalOrganic Letters
Volume3
Issue number26
DOIs
StatePublished - Dec 27 2001

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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