| Literature DB >> 19272776 |
Sukhdev Manku1, Martin Allan, Natalie Nguyen, Alain Ajamian, Jacques Rodrigue, Eric Therrien, James Wang, Tim Guo, Jubrail Rahil, Andrea J Petschner, Alina Nicolescu, Sylvain Lefebvre, Zuomei Li, Marielle Fournel, Jeffrey M Besterman, Robert Déziel, Amal Wahhab.
Abstract
We have recently reported on a novel class of histone deacetylase (HDAC) inhibitors bearing a sulfamide group as the zinc-binding unit. Herein, we report on the synthesis of sulfamide based inhibitors designed around a lysine scaffold and their structure-activity relationships against HDAC1 and HDAC6 isotypes as well as 293T cells. Our efforts led us to an improvement of the originally disclosed lysine-based sulfamide, 2a to compound 12h which has equal potency in enzyme and cell-based assays as well as enhanced metabolic stability and PK profile.Entities:
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Year: 2009 PMID： 19272776 DOI： 10.1016/j.bmcl.2009.02.075
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823