Synthesis of 7200 small molecules based on a substructural analysis of the histone deacetylase inhibitors trichostatin and trapoxin.
Org Lett
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| 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 tested for inhibitory activity and the 1,3-dioxane structure was shown to be compatible with HDAC inhibition. [structure: see text] |
| Year of Publication | 2001
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| Journal | Org Lett
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| Volume | 3
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| Issue | 26
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| Pages | 4239-42
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| Date Published | 2001 Dec 27
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| ISSN | 1523-7060
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| PubMed ID | 11784187
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| Grant list | GM 38627 / GM / NIGMS NIH HHS / United States
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