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Identification of a series of substituted 2-piperazinyl-5-pyrimidylhydroxamic acids as potent histone deacetylase inhibitors

2009; Elsevier BV; Volume: 20; Issue: 1 Linguagem: Inglês

10.1016/j.bmcl.2009.10.118

1464-3405

Patrick Angibaud, Kristof Van Emelen, Laurence Decrane, Sven Van Brandt, Peter ten Holte, Isabelle Pilatte, Bruno Roux, Virginie Poncelet, David Speybrouck, Laurence Quéguiner, Sandrine Gaurrand, Ann Mariën, Wim Floren, Lut Janssen, Marc Verdonck, Jacky Van Dun, Jacky Van Gompel, Ron Gilissen, Claire Mackie, Marc Du Jardin, Jozef Peeters, M. Noppe, Luc Van Hijfte, Eddy Freyne, Martin Pagé, Michel Janicot, Janine Arts,

Peptidase Inhibition and Analysis

Pursuing our efforts in designing 5-pyrimidylhydroxamic acid anti-cancer agents, we have identified a new series of potent histone deacetylase (HDAC) inhibitors. These compounds exhibit enzymatic HDAC inhibiting properties with IC(50) values in the nanomolar range and inhibit tumor cell proliferation at similar levels. Good solubility, moderate bioavailability, and promising in vivo activity in xenograft model made this series of compounds interesting starting points to design new potent HDAC inhibitors.