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Page 1
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.
Brough PA, Aherne W, Barril X, Borgognoni J, Boxall K, Cansfield JE, Cheung KM, Collins I, Davies NG, Drysdale MJ, Dymock B, Eccles SA, Finch H, Fink A, Hayes A, Howes R, Hubbard RE, James K, Jordan AM, Lockie A, Martins V, Massey A, Matthews TP, McDonald E, Northfield CJ, Pearl LH, Prodromou C, Ray S, Raynaud FI, Roughley SD, Sharp SY, Surgenor A, Walmsley DL, Webb P, Wood M, Workman P, Wright L. Brough PA, et al. Among authors: howes r. J Med Chem. 2008 Jan 24;51(2):196-218. doi: 10.1021/jm701018h. Epub 2007 Nov 20. J Med Chem. 2008. PMID: 18020435
4-Amino derivatives of the Hsp90 inhibitor CCT018159.
Barril X, Beswick MC, Collier A, Drysdale MJ, Dymock BW, Fink A, Grant K, Howes R, Jordan AM, Massey A, Surgenor A, Wayne J, Workman P, Wright L. Barril X, et al. Among authors: howes r. Bioorg Med Chem Lett. 2006 May 1;16(9):2543-8. doi: 10.1016/j.bmcl.2006.01.099. Epub 2006 Feb 9. Bioorg Med Chem Lett. 2006. PMID: 16480864
A fluorescence polarization assay for inhibitors of Hsp90.
Howes R, Barril X, Dymock BW, Grant K, Northfield CJ, Robertson AG, Surgenor A, Wayne J, Wright L, James K, Matthews T, Cheung KM, McDonald E, Workman P, Drysdale MJ. Howes R, et al. Anal Biochem. 2006 Mar 15;350(2):202-13. doi: 10.1016/j.ab.2005.12.023. Epub 2006 Jan 23. Anal Biochem. 2006. PMID: 16460658
Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.
Richardson CM, Williamson DS, Parratt MJ, Borgognoni J, Cansfield AD, Dokurno P, Francis GL, Howes R, Moore JD, Murray JB, Robertson A, Surgenor AE, Torrance CJ. Richardson CM, et al. Among authors: howes r. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1353-7. doi: 10.1016/j.bmcl.2005.11.048. Epub 2005 Dec 1. Bioorg Med Chem Lett. 2006. PMID: 16325401
Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping.
Richardson CM, Nunns CL, Williamson DS, Parratt MJ, Dokurno P, Howes R, Borgognoni J, Drysdale MJ, Finch H, Hubbard RE, Jackson PS, Kierstan P, Lentzen G, Moore JD, Murray JB, Simmonite H, Surgenor AE, Torrance CJ. Richardson CM, et al. Among authors: howes r. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3880-5. doi: 10.1016/j.bmcl.2007.04.110. Epub 2007 May 6. Bioorg Med Chem Lett. 2007. PMID: 17570665
Adenosine-derived inhibitors of 78 kDa glucose regulated protein (Grp78) ATPase: insights into isoform selectivity.
Macias AT, Williamson DS, Allen N, Borgognoni J, Clay A, Daniels Z, Dokurno P, Drysdale MJ, Francis GL, Graham CJ, Howes R, Matassova N, Murray JB, Parsons R, Shaw T, Surgenor AE, Terry L, Wang Y, Wood M, Massey AJ. Macias AT, et al. Among authors: howes r. J Med Chem. 2011 Jun 23;54(12):4034-41. doi: 10.1021/jm101625x. Epub 2011 May 20. J Med Chem. 2011. PMID: 21526763
Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.
Williamson DS, Parratt MJ, Bower JF, Moore JD, Richardson CM, Dokurno P, Cansfield AD, Francis GL, Hebdon RJ, Howes R, Jackson PS, Lockie AM, Murray JB, Nunns CL, Powles J, Robertson A, Surgenor AE, Torrance CJ. Williamson DS, et al. Among authors: howes r. Bioorg Med Chem Lett. 2005 Feb 15;15(4):863-7. doi: 10.1016/j.bmcl.2004.12.073. Bioorg Med Chem Lett. 2005. PMID: 15686876
179 results