Sort by
Items per page

Send to

Choose Destination

Search results

Items: 28


Discovery of Potent and Selective MRCK Inhibitors with Therapeutic Effect on Skin Cancer.

Unbekandt M, Belshaw S, Bower J, Clarke M, Cordes J, Crighton D, Croft DR, Drysdale MJ, Garnett MJ, Gill K, Gray C, Greenhalgh DA, Hall JAM, Konczal J, Lilla S, McArthur D, McConnell P, McDonald L, McGarry L, McKinnon H, McMenemy C, Mezna M, Morrice NA, Munro J, Naylor G, Rath N, Schüttelkopf AW, Sime M, Olson MF.

Cancer Res. 2018 Apr 15;78(8):2096-2114. doi: 10.1158/0008-5472.CAN-17-2870. Epub 2018 Jan 30.


Identification of novel, in vivo active Chk1 inhibitors utilizing structure guided drug design.

Massey AJ, Stokes S, Browne H, Foloppe N, Fiumana A, Scrace S, Fallowfield M, Bedford S, Webb P, Baker L, Christie M, Drysdale MJ, Wood M.

Oncotarget. 2015 Nov 3;6(34):35797-812. doi: 10.18632/oncotarget.5929.


Targeting conserved water molecules: design of 4-aryl-5-cyanopyrrolo[2,3-d]pyrimidine Hsp90 inhibitors using fragment-based screening and structure-based optimization.

Davies NG, Browne H, Davis B, Drysdale MJ, Foloppe N, Geoffrey S, Gibbons B, Hart T, Hubbard R, Jensen MR, Mansell H, Massey A, Matassova N, Moore JD, Murray J, Pratt R, Ray S, Robertson A, Roughley SD, Schoepfer J, Scriven K, Simmonite H, Stokes S, Surgenor A, Webb P, Wood M, Wright L, Brough P.

Bioorg Med Chem. 2012 Nov 15;20(22):6770-89. doi: 10.1016/j.bmc.2012.08.050. Epub 2012 Sep 4.


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.

J Med Chem. 2011 Jun 23;54(12):4034-41. doi: 10.1021/jm101625x. Epub 2011 May 20.


Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800.

Massey AJ, Schoepfer J, Brough PA, Brueggen J, Chène P, Drysdale MJ, Pfaar U, Radimerski T, Ruetz S, Schweitzer A, Wood M, Garcia-Echeverria C, Jensen MR.

Mol Cancer Ther. 2010 Apr;9(4):906-19. doi: 10.1158/1535-7163.MCT-10-0055. Epub 2010 Apr 6.


A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells.

Massey AJ, Williamson DS, Browne H, Murray JB, Dokurno P, Shaw T, Macias AT, Daniels Z, Geoffroy S, Dopson M, Lavan P, Matassova N, Francis GL, Graham CJ, Parsons R, Wang Y, Padfield A, Comer M, Drysdale MJ, Wood M.

Cancer Chemother Pharmacol. 2010 Aug;66(3):535-45. doi: 10.1007/s00280-009-1194-3. Epub 2009 Dec 13.


Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone.

Brough PA, Barril X, Borgognoni J, Chene P, Davies NG, Davis B, Drysdale MJ, Dymock B, Eccles SA, Garcia-Echeverria C, Fromont C, Hayes A, Hubbard RE, Jordan AM, Jensen MR, Massey A, Merrett A, Padfield A, Parsons R, Radimerski T, Raynaud FI, Robertson A, Roughley SD, Schoepfer J, Simmonite H, Sharp SY, Surgenor A, Valenti M, Walls S, Webb P, Wood M, Workman P, Wright L.

J Med Chem. 2009 Aug 13;52(15):4794-809. doi: 10.1021/jm900357y.


Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design.

Williamson DS, Borgognoni J, Clay A, Daniels Z, Dokurno P, Drysdale MJ, Foloppe N, Francis GL, Graham CJ, Howes R, Macias AT, Murray JB, Parsons R, Shaw T, Surgenor AE, Terry L, Wang Y, Wood M, Massey AJ.

J Med Chem. 2009 Mar 26;52(6):1510-3. doi: 10.1021/jm801627a.


Medicinal chemistry of Hsp90 inhibitors.

Drysdale MJ, Brough PA.

Curr Top Med Chem. 2008;8(10):859-68. Review.


NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models.

Jensen MR, Schoepfer J, Radimerski T, Massey A, Guy CT, Brueggen J, Quadt C, Buckler A, Cozens R, Drysdale MJ, Garcia-Echeverria C, Chène P.

Breast Cancer Res. 2008;10(2):R33. doi: 10.1186/bcr1996. Epub 2008 Apr 22.


NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis.

Eccles SA, Massey A, Raynaud FI, Sharp SY, Box G, Valenti M, Patterson L, de Haven Brandon A, Gowan S, Boxall F, Aherne W, Rowlands M, Hayes A, Martins V, Urban F, Boxall K, Prodromou C, Pearl L, James K, Matthews TP, Cheung KM, Kalusa A, Jones K, McDonald E, Barril X, Brough PA, Cansfield JE, Dymock B, Drysdale MJ, Finch H, Howes R, Hubbard RE, Surgenor A, Webb P, Wood M, Wright L, Workman P.

Cancer Res. 2008 Apr 15;68(8):2850-60. doi: 10.1158/0008-5472.CAN-07-5256.


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.

J Med Chem. 2008 Jan 24;51(2):196-218. Epub 2007 Nov 20.


The SeeDs approach: integrating fragments into drug discovery.

Hubbard RE, Davis B, Chen I, Drysdale MJ.

Curr Top Med Chem. 2007;7(16):1568-81. Review.


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.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3880-5. Epub 2007 May 6.


Targeting Hsp90 for the treatment of cancer.

Drysdale MJ, Brough PA, Massey A, Jensen MR, Schoepfer J.

Curr Opin Drug Discov Devel. 2006 Jul;9(4):483-95. Review.


Discovery and development of pyrazole-scaffold Hsp90 inhibitors.

McDonald E, Jones K, Brough PA, Drysdale MJ, Workman P.

Curr Top Med Chem. 2006;6(11):1193-203. Review.


Preclinical pharmacokinetics and metabolism of a novel diaryl pyrazole resorcinol series of heat shock protein 90 inhibitors.

Smith NF, Hayes A, James K, Nutley BP, McDonald E, Henley A, Dymock B, Drysdale MJ, Raynaud FI, Workman P.

Mol Cancer Ther. 2006 Jun;5(6):1628-37.


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.

Bioorg Med Chem Lett. 2006 May 1;16(9):2543-8. Epub 2006 Feb 9.


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.

Anal Biochem. 2006 Mar 15;350(2):202-13. Epub 2006 Jan 23.


3-(5-Chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone.

Brough PA, Barril X, Beswick M, Dymock BW, Drysdale MJ, Wright L, Grant K, Massey A, Surgenor A, Workman P.

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5197-201. Epub 2005 Oct 5.


Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.

Dymock BW, Barril X, Brough PA, Cansfield JE, Massey A, McDonald E, Hubbard RE, Surgenor A, Roughley SD, Webb P, Workman P, Wright L, Drysdale MJ.

J Med Chem. 2005 Jun 30;48(13):4212-5.


Structure-based drug design targeting an inactive RNA conformation: exploiting the flexibility of HIV-1 TAR RNA.

Murchie AI, Davis B, Isel C, Afshar M, Drysdale MJ, Bower J, Potter AJ, Starkey ID, Swarbrick TM, Mirza S, Prescott CD, Vaglio P, Aboul-ela F, Karn J.

J Mol Biol. 2004 Feb 20;336(3):625-38.


RNA as a drug target.

Drysdale MJ, Lentzen G, Matassova N, Murchie AI, Aboul-Ela F, Afshar M.

Prog Med Chem. 2002;39:73-119. Review.


The carbenoid approach to peptide synthesis.

Buck RT, Clarke PA, Coe DM, Drysdale MJ, Ferris L, Haigh D, Moody CJ, Pearson ND, Swann E.

Chemistry. 2000 Jun 16;6(12):2160-7.


Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine.

Young RJ, Beams RM, Carter K, Clark HA, Coe DM, Chambers CL, Davies PI, Dawson J, Drysdale MJ, Franzman KW, French C, Hodgson ST, Hodson HF, Kleanthous S, Rider P, Sanders D, Sawyer DA, Scott KJ, Shearer BG, Stocker R, Smith S, Tackley MC, Knowles RG.

Bioorg Med Chem Lett. 2000 Mar 20;10(6):597-600.


S-aryl cysteine S,S-dioxides as inhibitors of mammalian kynureninase.

Drysdale MJ, Reinhard JF.

Bioorg Med Chem Lett. 1998 Jan 20;8(2):133-8.


Supplemental Content

Loading ...
Support Center