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Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
Moffat D, Patel S, Day F, Belfield A, Donald A, Rowlands M, Wibawa J, Brotherton D, Stimson L, Clark V, Owen J, Bawden L, Box G, Bone E, Mortenson P, Hardcastle A, van Meurs S, Eccles S, Raynaud F, Aherne W. Moffat D, et al. J Med Chem. 2010 Dec 23;53(24):8663-78. doi: 10.1021/jm101177s. Epub 2010 Nov 16. J Med Chem. 2010. PMID: 21080647
Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases.
Donald AD, Clark VL, Patel S, Day FA, Rowlands MG, Wibata J, Stimson L, Hardcastle A, Eccles SA, McNamara D, Needham LA, Raynaud FI, Aherne W, Moffat DF. Donald AD, et al. Among authors: moffat df. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6657-60. doi: 10.1016/j.bmcl.2010.09.016. Epub 2010 Sep 21. Bioorg Med Chem Lett. 2010. PMID: 20884208
Drug targeting to monocytes and macrophages using esterase-sensitive chemical motifs.
Needham LA, Davidson AH, Bawden LJ, Belfield A, Bone EA, Brotherton DH, Bryant S, Charlton MH, Clark VL, Davies SJ, Donald A, Day FA, Krige D, Legris V, McDermott J, McGovern Y, Owen J, Patel SR, Pintat S, Testar RJ, Wells GM, Moffat D, Drummond AH. Needham LA, et al. Among authors: moffat d. J Pharmacol Exp Ther. 2011 Oct;339(1):132-42. doi: 10.1124/jpet.111.183640. Epub 2011 Jul 21. J Pharmacol Exp Ther. 2011. PMID: 21778281
Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin.
Huertas D, Soler M, Moreto J, Villanueva A, Martinez A, Vidal A, Charlton M, Moffat D, Patel S, McDermott J, Owen J, Brotherton D, Krige D, Cuthill S, Esteller M. Huertas D, et al. Among authors: moffat d. Oncogene. 2012 Mar 15;31(11):1408-18. doi: 10.1038/onc.2011.335. Epub 2011 Aug 1. Oncogene. 2012. PMID: 21804608 Free PMC article.
297 results