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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: besterman jm. Mol Cancer Ther. 2008 Apr;7(4):759-68. doi: 10.1158/1535-7163.MCT-07-2026. Mol Cancer Ther. 2008. PMID: 18413790
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. Among authors: besterman jm. 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.
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: besterman jm. 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
Phase I study of MGCD0103 given as a three-times-per-week oral dose in patients with advanced solid tumors.
Siu LL, Pili R, Duran I, Messersmith WA, Chen EX, Sullivan R, MacLean M, King S, Brown S, Reid GK, Li Z, Kalita AM, Laille EJ, Besterman JM, Martell RE, Carducci MA. Siu LL, et al. Among authors: besterman jm. J Clin Oncol. 2008 Apr 20;26(12):1940-7. doi: 10.1200/JCO.2007.14.5730. J Clin Oncol. 2008. PMID: 18421048 Free PMC article. Clinical Trial.
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: besterman jm. 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. Among authors: besterman jm. 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
(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: besterman jm. 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
Sulfamides as novel histone deacetylase inhibitors.
Wahhab A, Smil D, Ajamian A, Allan M, Chantigny Y, Therrien E, Nguyen N, Manku S, Leit S, Rahil J, Petschner AJ, Lu AH, Nicolescu A, Lefebvre S, Montcalm S, Fournel M, Yan TP, Li Z, Besterman JM, Déziel R. Wahhab A, et al. Among authors: besterman jm. Bioorg Med Chem Lett. 2009 Jan 15;19(2):336-40. doi: 10.1016/j.bmcl.2008.11.081. Epub 2008 Nov 27. Bioorg Med Chem Lett. 2009. PMID: 19084395
83 results