| Literature DB >> 17761416 |
Christopher L Hamblett1, Joey L Methot, Dawn M Mampreian, David L Sloman, Matthew G Stanton, Astrid M Kral, Judith C Fleming, Jonathan C Cruz, Melissa Chenard, Nicole Ozerova, Anna M Hitz, Hongmei Wang, Sujal V Deshmukh, Naim Nazef, Andreas Harsch, Bethany Hughes, William K Dahlberg, Alex A Szewczak, Richard E Middleton, Ralph T Mosley, J Paul Secrist, Thomas A Miller.
Abstract
This communication highlights the development of a nicotinamide series of histone deacetylase inhibitors within the benzamide structural class. Extensive exploration around the nicotinamide core led to the discovery of a class I selective HDAC inhibitor that possesses excellent intrinsic and cell-based potency, acceptable ancillary pharmacology, favorable pharmacokinetics, sustained pharmacodynamics in vitro, and achieves in vivo efficacy in an HCT116 xenograft model.Entities:
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Year: 2007 PMID： 17761416 DOI： 10.1016/j.bmcl.2007.08.023
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823