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Page 1
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. Among authors: kalita a. J Med Chem. 2008 Jul 24;51(14):4072-5. doi: 10.1021/jm800251w. Epub 2008 Jun 21. J Med Chem. 2008. PMID: 18570366
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
Bouchain G, Leit S, Frechette S, Khalil EA, Lavoie R, Moradei O, Woo SH, Fournel M, Yan PT, Kalita A, Trachy-Bourget MC, Beaulieu C, Li Z, Robert MF, MacLeod AR, Besterman JM, Delorme D. Bouchain G, et al. Among authors: kalita a. J Med Chem. 2003 Feb 27;46(5):820-30. doi: 10.1021/jm020377a. J Med Chem. 2003. PMID: 12593661
(2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors.
Vaisburg A, Bernstein N, Frechette S, Allan M, Abou-Khalil E, Leit S, Moradei O, Bouchain G, Wang J, Woo SH, Fournel M, Yan PT, Trachy-Bourget MC, Kalita A, Beaulieu C, Li Z, MacLeod AR, Besterman JM, Delorme D. Vaisburg A, et al. Among authors: kalita a. Bioorg Med Chem Lett. 2004 Jan 5;14(1):283-7. doi: 10.1016/j.bmcl.2003.08.083. Bioorg Med Chem Lett. 2004. PMID: 14684344
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. Among authors: kalita a. 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
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. Among authors: kalita a. 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
4-(Heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs as a novel class of histone deacetylase inhibitors.
Fréchette S, Leit S, Woo SH, Lapointe G, Jeannotte G, Moradei O, Paquin I, Bouchain G, Raeppel S, Gaudette F, Zhou N, Vaisburg A, Fournel M, Yan PT, Trachy-Bourget MC, Kalita A, Robert MF, Lu A, Rahil J, Robert Macleod A, Besterman JM, Li Z, Delorme D. Fréchette S, et al. Among authors: kalita a. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1502-6. doi: 10.1016/j.bmcl.2007.12.057. Epub 2007 Dec 25. Bioorg Med Chem Lett. 2008. PMID: 18207391
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. Among authors: kalita a. Mol Cancer Ther. 2008 Apr;7(4):759-68. doi: 10.1158/1535-7163.MCT-07-2026. Mol Cancer Ther. 2008. PMID: 18413790
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. Among authors: kalita a. 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
165 results