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463 results

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Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design.
Woodhead AJ, Angove H, Carr MG, Chessari G, Congreve M, Coyle JE, Cosme J, Graham B, Day PJ, Downham R, Fazal L, Feltell R, Figueroa E, Frederickson M, Lewis J, McMenamin R, Murray CW, O'Brien MA, Parra L, Patel S, Phillips T, Rees DC, Rich S, Smith DM, Trewartha G, Vinkovic M, Williams B, Woolford AJ. Woodhead AJ, et al. Among authors: rees dc. J Med Chem. 2010 Aug 26;53(16):5956-69. doi: 10.1021/jm100060b. J Med Chem. 2010. PMID: 20662534
Experiences in fragment-based drug discovery.
Murray CW, Verdonk ML, Rees DC. Murray CW, et al. Among authors: rees dc. Trends Pharmacol Sci. 2012 May;33(5):224-32. doi: 10.1016/j.tips.2012.02.006. Epub 2012 Mar 27. Trends Pharmacol Sci. 2012. PMID: 22459076
Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors.
Cho YS, Angove H, Brain C, Chen CH, Cheng H, Cheng R, Chopra R, Chung K, Congreve M, Dagostin C, Davis DJ, Feltell R, Giraldes J, Hiscock SD, Kim S, Kovats S, Lagu B, Lewry K, Loo A, Lu Y, Luzzio M, Maniara W, McMenamin R, Mortenson PN, Benning R, O'Reilly M, Rees DC, Shen J, Smith T, Wang Y, Williams G, Woolford AJ, Wrona W, Xu M, Yang F, Howard S. Cho YS, et al. Among authors: rees dc. ACS Med Chem Lett. 2012 May 17;3(6):445-9. doi: 10.1021/ml200241a. eCollection 2012 Jun 14. ACS Med Chem Lett. 2012. PMID: 24900493 Free PMC article.
Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP.
Chessari G, Buck IM, Day JE, Day PJ, Iqbal A, Johnson CN, Lewis EJ, Martins V, Miller D, Reader M, Rees DC, Rich SJ, Tamanini E, Vitorino M, Ward GA, Williams PA, Williams G, Wilsher NE, Woolford AJ. Chessari G, et al. Among authors: rees dc. J Med Chem. 2015 Aug 27;58(16):6574-88. doi: 10.1021/acs.jmedchem.5b00706. Epub 2015 Aug 7. J Med Chem. 2015. PMID: 26218264
Fragment-to-Lead Medicinal Chemistry Publications in 2016.
Johnson CN, Erlanson DA, Jahnke W, Mortenson PN, Rees DC. Johnson CN, et al. Among authors: rees dc. J Med Chem. 2018 Mar 8;61(5):1774-1784. doi: 10.1021/acs.jmedchem.7b01298. Epub 2017 Oct 31. J Med Chem. 2018. PMID: 29087197 Review.
Fragment-based lead discovery.
Rees DC, Congreve M, Murray CW, Carr R. Rees DC, et al. Nat Rev Drug Discov. 2004 Aug;3(8):660-72. doi: 10.1038/nrd1467. Nat Rev Drug Discov. 2004. PMID: 15286733 Review. No abstract available.
Fragment-based lead discovery: leads by design.
Carr RA, Congreve M, Murray CW, Rees DC. Carr RA, et al. Among authors: rees dc. Drug Discov Today. 2005 Jul 15;10(14):987-92. doi: 10.1016/S1359-6446(05)03511-7. Drug Discov Today. 2005. PMID: 16023057 Review.
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