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Page 1
Design, Synthesis, and Evaluation of Inhibitors of Hedgehog Acyltransferase.
Ritzefeld M, Zhang L, Xiao Z, Andrei SA, Boyd O, Masumoto N, Rodgers UR, Artelsmair M, Sefer L, Hayes A, Gavriil ES, Raynaud FI, Burke R, Blagg J, Rzepa HS, Siebold C, Magee AI, Lanyon-Hogg T, Tate EW. Ritzefeld M, et al. Among authors: hayes a. J Med Chem. 2024 Jan 25;67(2):1061-1078. doi: 10.1021/acs.jmedchem.3c01363. Epub 2024 Jan 10. J Med Chem. 2024. PMID: 38198226 Free PMC 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: hayes a. J Med Chem. 2008 Jan 24;51(2):196-218. doi: 10.1021/jm701018h. Epub 2007 Nov 20. J Med Chem. 2008. PMID: 18020435
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: hayes a. J Med Chem. 2008 Sep 25;51(18):5522-32. doi: 10.1021/jm800295d. J Med Chem. 2008. PMID: 18754654
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. Brough PA, et al. Among authors: hayes a. J Med Chem. 2009 Aug 13;52(15):4794-809. doi: 10.1021/jm900357y. J Med Chem. 2009. PMID: 19610616
Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements.
Large JM, Torr JE, Raynaud FI, Clarke PA, Hayes A, Stefano Fd, Urban F, Shuttleworth SJ, Saghir N, Sheldrake P, Workman P, McDonald E. Large JM, et al. Among authors: hayes a. Bioorg Med Chem. 2011 Jan 15;19(2):836-51. doi: 10.1016/j.bmc.2010.12.006. Epub 2010 Dec 9. Bioorg Med Chem. 2011. PMID: 21216151
1,973 results