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

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.

Hybrids of known histone deacetylases inhibitors (HDI) based on indanones were synthesized. Several alkylated indanones were obtained as hydroxamic acid and aminobenzamides derivatives and evaluated for their antiproliferative activity towards non small lung cancer cell line H661.Figure optionsDownload as PowerPoint slide