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232 results

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Page 1
Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.
Schiemann K, Mallinger A, Wienke D, Esdar C, Poeschke O, Busch M, Rohdich F, Eccles SA, Schneider R, Raynaud FI, Czodrowski P, Musil D, Schwarz D, Urbahns K, Blagg J. Schiemann K, et al. Among authors: eccles sa. Bioorg Med Chem Lett. 2016 Mar 1;26(5):1443-51. doi: 10.1016/j.bmcl.2016.01.062. Epub 2016 Jan 22. Bioorg Med Chem Lett. 2016. PMID: 26852363
In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202.
Raynaud FI, Whittaker SR, Fischer PM, McClue S, Walton MI, Barrie SE, Garrett MD, Rogers P, Clarke SJ, Kelland LR, Valenti M, Brunton L, Eccles S, Lane DP, Workman P. Raynaud FI, et al. Clin Cancer Res. 2005 Jul 1;11(13):4875-87. doi: 10.1158/1078-0432.CCR-04-2264. Clin Cancer Res. 2005. PMID: 16000586
The phosphoinositide-specific phospholipase C inhibitor U73122 (1-(6-((17beta-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione) spontaneously forms conjugates with common components of cell culture medium.
Wilsher NE, Court WJ, Ruddle R, Newbatt YM, Aherne W, Sheldrake PW, Jones NP, Katan M, Eccles SA, Raynaud FI. Wilsher NE, et al. Among authors: eccles sa. Drug Metab Dispos. 2007 Jul;35(7):1017-22. doi: 10.1124/dmd.106.014498. Epub 2007 Apr 2. Drug Metab Dispos. 2007. PMID: 17403917
Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases.
Raynaud FI, Eccles S, Clarke PA, Hayes A, Nutley B, Alix S, Henley A, Di-Stefano F, Ahmad Z, Guillard S, Bjerke LM, Kelland L, Valenti M, Patterson L, Gowan S, de Haven Brandon A, Hayakawa M, Kaizawa H, Koizumi T, Ohishi T, Patel S, Saghir N, Parker P, Waterfield M, Workman P. Raynaud FI, et al. Cancer Res. 2007 Jun 15;67(12):5840-50. doi: 10.1158/0008-5472.CAN-06-4615. Cancer Res. 2007. PMID: 17575152 Free article.
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: eccles sa. J Med Chem. 2008 Jan 24;51(2):196-218. doi: 10.1021/jm701018h. Epub 2007 Nov 20. J Med Chem. 2008. PMID: 18020435
An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models.
Banerji U, Sain N, Sharp SY, Valenti M, Asad Y, Ruddle R, Raynaud F, Walton M, Eccles SA, Judson I, Jackman AL, Workman P. Banerji U, et al. Among authors: eccles sa. Cancer Chemother Pharmacol. 2008 Oct;62(5):769-78. doi: 10.1007/s00280-007-0662-x. Epub 2008 Jan 10. Cancer Chemother Pharmacol. 2008. PMID: 18193424
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. Eccles SA, et al. Cancer Res. 2008 Apr 15;68(8):2850-60. doi: 10.1158/0008-5472.CAN-07-5256. Cancer Res. 2008. PMID: 18413753
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer.
Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, Chuckowree IS, Clarke PA, Depledge P, Eccles SA, Friedman LS, Hayes A, Hancox TC, Kugendradas A, Lensun L, Moore P, Olivero AG, Pang J, Patel S, Pergl-Wilson GH, Raynaud FI, Robson A, Saghir N, Salphati L, Sohal S, Ultsch MH, Valenti M, Wallweber HJ, Wan NC, Wiesmann C, Workman P, Zhyvoloup A, Zvelebil MJ, Shuttleworth SJ. Folkes AJ, et al. Among authors: eccles sa. J Med Chem. 2008 Sep 25;51(18):5522-32. doi: 10.1021/jm800295d. J Med Chem. 2008. PMID: 18754654
232 results