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Antiproliferative activities of a library of hybrids between indanones and HDAC inhibitor SAHA and MS-275 analogues

2007; Elsevier BV; Volume: 17; Issue: 22 Linguagem: Inglês

10.1016/j.bmcl.2007.09.041

1464-3405

Cédric Charrier, Joëlle Roche, Jean‐Pierre Gesson, Philìppe Bertrand,

Epigenetics and DNA Methylation

New compounds derived from inhibitors of histone deacetylases (HDACs) have been synthesized and their antiproliferative activities towards non small lung cancer cell line H661 evaluated. Their design is based on hybrids between indanones to limit conformational mobility and other known HDAC inhibitors (SAHA, MS-275). The synthesis of these new derivatives was achieved by alkylation of appropriate indanones to introduce the side chain bearing a terminal ester group, the latter being a precursor of hydroxamic acid and aminobenzamide derivatives. These new analogues were found to be moderately active to inhibit H661 cell proliferation.