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ID: ALA1136247

Journal: Bioorg Med Chem Lett

Title: Alpha-keto amides as inhibitors of histone deacetylase.

Authors: Wada CK, Frey RR, Ji Z, Curtin ML, Garland RB, Holms JH, Li J, Pease LJ, Guo J, Glaser KB, Marcotte PA, Richardson PL, Murphy SS, Bouska JJ, Tapang P, Magoc TJ, Albert DH, Davidsen SK, Michaelides MR.

Abstract: Alpha-keto ester and amides were found to be potent inhibitors of histone deacetylase. Nanomolar inhibitors against the isolated enzyme and sub-micromolar inhibitors of cellular proliferation were obtained. The alpha-keto amide 30 also exhibited significant anti-tumor effects in an in vivo tumor model.

CiteXplore: 12951120

DOI: 10.1016/s0960-894x(03)00685-1