【文章名】Discovery of N-(2-Aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzam ide (MGCD0103), an Orally Active Histone Deacetylase Inhibitor.
[摘要]：The design, synthesis, and biol. evaluation of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzam ide (MGCD0103) (I) is described. Compd. I is an isotype-selective small mol. histone deacetylase (HDAC) inhibitor that selectively inhibits HDACs 1-3 and 11 at submicromolar concns. in vitro. I blocks cancer cell proliferation and induces histone acetylation, p21cip/waf1 protein expression, cell-cycle arrest, and apoptosis. I is orally bioavailable, has significant antitumor activity in vivo, has entered clin. trials, and shows promise as an anticancer drug.
