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Page 1
Phase 1 study of the oral isotype specific histone deacetylase inhibitor MGCD0103 in leukemia.
Garcia-Manero G, Assouline S, Cortes J, Estrov Z, Kantarjian H, Yang H, Newsome WM, Miller WH Jr, Rousseau C, Kalita A, Bonfils C, Dubay M, Patterson TA, Li Z, Besterman JM, Reid G, Laille E, Martell RE, Minden M. Garcia-Manero G, et al. Blood. 2008 Aug 15;112(4):981-9. doi: 10.1182/blood-2007-10-115873. Epub 2008 May 21. Blood. 2008. PMID: 18495956 Free PMC article. Clinical Trial.
MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo.
Fournel M, Bonfils C, Hou Y, Yan PT, Trachy-Bourget MC, Kalita A, Liu J, Lu AH, Zhou NZ, Robert MF, Gillespie J, Wang JJ, Ste-Croix H, Rahil J, Lefebvre S, Moradei O, Delorme D, Macleod AR, Besterman JM, Li Z. Fournel M, et al. Mol Cancer Ther. 2008 Apr;7(4):759-68. doi: 10.1158/1535-7163.MCT-07-2026. Mol Cancer Ther. 2008. PMID: 18413790
Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor.
Zhou N, Moradei O, Raeppel S, Leit S, Frechette S, Gaudette F, Paquin I, Bernstein N, Bouchain G, Vaisburg A, Jin Z, Gillespie J, Wang J, Fournel M, Yan PT, Trachy-Bourget MC, Kalita A, Lu A, Rahil J, MacLeod AR, Li Z, Besterman JM, Delorme D. Zhou N, et al. J Med Chem. 2008 Jul 24;51(14):4072-5. doi: 10.1021/jm800251w. Epub 2008 Jun 21. J Med Chem. 2008. PMID: 18570366
Substituted N-(2-aminophenyl)-benzamides, (E)-N-(2-aminophenyl)-acrylamides and their analogues: novel classes of histone deacetylase inhibitors.
Moradei O, Leit S, Zhou N, Fréchette S, Paquin I, Raeppel S, Gaudette F, Bouchain G, Woo SH, Vaisburg A, Fournel M, Kalita A, Lu A, Trachy-Bourget MC, Yan PT, Liu J, Li Z, Rahil J, MacLeod AR, Besterman JM, Delorme D. Moradei O, et al. Bioorg Med Chem Lett. 2006 Aug 1;16(15):4048-52. doi: 10.1016/j.bmcl.2006.05.005. Epub 2006 May 18. Bioorg Med Chem Lett. 2006. PMID: 16713259
SAR and biological evaluation of analogues of a small molecule histone deacetylase inhibitor N-(2-aminophenyl)-4-((4-(pyridin-3-yl)pyrimidin-2-ylamino)methyl)benzamide (MGCD0103).
Raeppel S, Zhou N, Gaudette F, Leit S, Paquin I, Larouche G, Moradei O, Fréchette S, Isakovic L, Delorme D, Fournel M, Kalita A, Lu A, Trachy-Bourget MC, Yan PT, Liu J, Rahil J, Wang J, Besterman JM, Murakami K, Li Z, Vaisburg A. Raeppel S, et al. Bioorg Med Chem Lett. 2009 Feb 1;19(3):644-9. doi: 10.1016/j.bmcl.2008.12.048. Epub 2008 Dec 24. Bioorg Med Chem Lett. 2009. PMID: 19114304
Design and synthesis of 4-[(s-triazin-2-ylamino)methyl]-N-(2-aminophenyl)-benzamides and their analogues as a novel class of histone deacetylase inhibitors.
Paquin I, Raeppel S, Leit S, Gaudette F, Zhou N, Moradei O, Saavedra O, Bernstein N, Raeppel F, Bouchain G, Fréchette S, Woo SH, Vaisburg A, Fournel M, Kalita A, Robert MF, Lu A, Trachy-Bourget MC, Yan PT, Liu J, Rahil J, MacLeod AR, Besterman JM, Li Z, Delorme D. Paquin I, et al. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1067-71. doi: 10.1016/j.bmcl.2007.12.009. Epub 2007 Dec 10. Bioorg Med Chem Lett. 2008. PMID: 18160287
12 results