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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
SAR around (l)-S-adenosyl-l-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes.
Saavedra OM, Isakovic L, Llewellyn DB, Zhan L, Bernstein N, Claridge S, Raeppel F, Vaisburg A, Elowe N, Petschner AJ, Rahil J, Beaulieu N, MacLeod AR, Delorme D, Besterman JM, Wahhab A. Saavedra OM, et al. Among authors: besterman jm. Bioorg Med Chem Lett. 2009 May 15;19(10):2747-51. doi: 10.1016/j.bmcl.2009.03.113. Epub 2009 Mar 28. Bioorg Med Chem Lett. 2009. PMID: 19362833
Phase I and pharmacologic study of the human DNA methyltransferase antisense oligodeoxynucleotide MG98 given as a 21-day continuous infusion every 4 weeks.
Davis AJ, Gelmon KA, Siu LL, Moore MJ, Britten CD, Mistry N, Klamut H, D'Aloisio S, MacLean M, Wainman N, Ayers D, Firby P, Besterman JM, Reid GK, Eisenhauer EA. Davis AJ, et al. Among authors: besterman jm. Invest New Drugs. 2003 Feb;21(1):85-97. doi: 10.1023/a:1022976528441. Invest New Drugs. 2003. PMID: 12795533 Clinical Trial.
(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
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
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
Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors.
Isakovic L, Saavedra OM, Llewellyn DB, Claridge S, Zhan L, Bernstein N, Vaisburg A, Elowe N, Petschner AJ, Rahil J, Beaulieu N, Gauthier F, MacLeod AR, Delorme D, Besterman JM, Wahhab A. Isakovic L, et al. Among authors: besterman jm. Bioorg Med Chem Lett. 2009 May 15;19(10):2742-6. doi: 10.1016/j.bmcl.2009.03.132. Epub 2009 Mar 28. Bioorg Med Chem Lett. 2009. PMID: 19364644
83 results