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247 results

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Page 1
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. Among authors: hardcastle a. 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: hardcastle a. 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
Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues.
Sharp SY, Prodromou C, Boxall K, Powers MV, Holmes JL, Box G, Matthews TP, Cheung KM, Kalusa A, James K, Hayes A, Hardcastle A, Dymock B, Brough PA, Barril X, Cansfield JE, Wright L, Surgenor A, Foloppe N, Hubbard RE, Aherne W, Pearl L, Jones K, McDonald E, Raynaud F, Eccles S, Drysdale M, Workman P. Sharp SY, et al. Among authors: hardcastle a. Mol Cancer Ther. 2007 Apr;6(4):1198-211. doi: 10.1158/1535-7163.MCT-07-0149. Mol Cancer Ther. 2007. PMID: 17431102 Free article.
Assays for HSP90 and inhibitors.
Aherne W, Maloney A, Prodromou C, Rowlands MG, Hardcastle A, Boxall K, Clarke P, Walton MI, Pearl L, Workman P. Aherne W, et al. Among authors: hardcastle a. Methods Mol Med. 2003;85:149-61. doi: 10.1385/1-59259-380-1:149. Methods Mol Med. 2003. PMID: 12710206 Review. No abstract available.
A phase I study of the heat shock protein 90 inhibitor alvespimycin (17-DMAG) given intravenously to patients with advanced solid tumors.
Pacey S, Wilson RH, Walton M, Eatock MM, Hardcastle A, Zetterlund A, Arkenau HT, Moreno-Farre J, Banerji U, Roels B, Peachey H, Aherne W, de Bono JS, Raynaud F, Workman P, Judson I. Pacey S, et al. Among authors: hardcastle a. Clin Cancer Res. 2011 Mar 15;17(6):1561-70. doi: 10.1158/1078-0432.CCR-10-1927. Epub 2011 Jan 28. Clin Cancer Res. 2011. PMID: 21278242 Free PMC article. Clinical Trial.
247 results