Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform |
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| Institution: | 1. Medical Genetics Unit, IRCCS Casa Sollievo Della Sofferenza Hospital, 71013 San Giovanni Rotondo, Italy;2. Telethon Institute of Genetics and Medicine, Via P. Castellino 111, 80131 Naples, Italy;3. CEINGE Advanced Biotechnology and Department of Organic Chemistry and Biochemistry, Federico II University, 80131 Napoli, Italy;4. Scienze della Riproduzione e dello Sviluppo, University of Trieste, Italy |
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| Abstract: | Acyl derivatives of 4-(aminomethyl)-N-hydroxybenzamide are potent sub-type selective HDAC6 inhibitors. Constrained heterocyclic analogs based on 1,2,3,4-tetrahydropyrrolo1,2-a]pyrazine show further enhanced HDAC6 selectivity and inhibitory activity in cells. Homology models suggest that the heterocyclic spacer can more effectively access the wider catalytic channel of HDAC6 compared to other HDAC sub-types. |
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| Keywords: | Histone deacetylase HDAC6 selective Hydroxamic acid Acetyl tubulin |
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