| Literature DB >> 18570366 |
Nancy Zhou1, Oscar Moradei, Stephane Raeppel, Silvana Leit, Sylvie Frechette, Frederic Gaudette, Isabelle Paquin, Naomy Bernstein, Giliane Bouchain, Arkadii Vaisburg, Zhiyun Jin, Jeff Gillespie, James Wang, Marielle Fournel, Pu T Yan, Marie-Claude Trachy-Bourget, Ann Kalita, Aihua Lu, Jubrail Rahil, A Robert MacLeod, Zuomei Li, Jeffrey M Besterman, Daniel Delorme.
Abstract
The design, synthesis, and biological evaluation of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide 8 (MGCD0103) is described. Compound 8 is an isotype-selective small molecule histone deacetylase (HDAC) inhibitor that selectively inhibits HDACs 1-3 and 11 at submicromolar concentrations in vitro. 8 blocks cancer cell proliferation and induces histone acetylation, p21 (cip/waf1) protein expression, cell-cycle arrest, and apoptosis. 8 is orally bioavailable, has significant antitumor activity in vivo, has entered clinical trials, and shows promise as an anticancer drug.Entities:
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Year: 2008 PMID： 18570366 DOI： 10.1021/jm800251w
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446