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

…, JC Wong, CM Grozinger, SL Schreiber

Index: Sternson; Wong; Grozinger; Schreiber Organic letters, 2001 , vol. 3, # 26 p. 4239 - 4242

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Citation Number: 149

Abstract

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 ...