Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 1, Issue 8, Pages 411-415Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml1001163
Keywords
HDAC inhibitors; hydroxamic acid; retinoic acid; antiproliferative effect; differentiation
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Funding
- Associazione Italiana per la Ricerca contro il Cancro (AIRC)
- Fondazione Italo Monzino
- Ministero della Ricerca (Progetti Finalizzati)
- Menarini Industrie Farmaceutiche Riunite
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Histone deacetylases are promising molecular targets for the development of antitumor agents. A novel series of histone deacetylase inhibitors of the hydroxamic acid type were synthesized for structure-activity studies. Thirteen tricyclic dibenzo diazepine, -oxazepine, and -thiazepine analogues were studied and shown to induce variable degrees of histone H3/H4 and tubulinacetylation in a cellular model of myeloid leukemia sensitive to all-trans retinoic acid (ATRA). Multiparametric correlations between acetylation of the three substrates, tumor cell growth inhibition, and ATRA-dependent cytodifferentiation were performed, providing information on the chemical functionalities governing these activities. For two analogues, antitumor activity in the animal was demonstrated.
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