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Design, synthesis and structure-activity relationships of (indo-3-yl) heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate.
Ratcliffe P, Adam JM, Baker J, Bursi R, Campbell R, Clark JK, Cottney JE, Deehan M, Easson AM, Ecker D, Edwards D, Epemolu O, Evans L, Fields R, Francis S, Harradine P, Jeremiah F, Kiyoi T, McArthur D, Morrison A, Passier P, Pick J, Schnabel PG, Schulz J, Steinbrede H, Walker G, Westwood P, Wishart G, Udo de Haes J. Ratcliffe P, et al. Among authors: mcarthur d. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2541-6. doi: 10.1016/j.bmcl.2011.02.023. Epub 2011 Feb 12. Bioorg Med Chem Lett. 2011. PMID: 21411321
Design, synthesis, and structure-activity relationships of indole-3-heterocycles as agonists of the CB1 receptor.
Morrison AJ, Adam JM, Baker JA, Campbell RA, Clark JK, Cottney JE, Deehan M, Easson AM, Fields R, Francis S, Jeremiah F, Keddie N, Kiyoi T, McArthur DR, Meyer K, Ratcliffe PD, Schulz J, Wishart G, Yoshiizumi K. Morrison AJ, et al. Among authors: mcarthur dr. Bioorg Med Chem Lett. 2011 Jan 1;21(1):506-9. doi: 10.1016/j.bmcl.2010.10.093. Epub 2010 Oct 25. Bioorg Med Chem Lett. 2011. PMID: 21075630
Rapid access towards follow-up NOP receptor agonists using a knowledge based approach.
Palin R, Clark JK, Evans L, Feilden H, Fletcher D, Hamilton NM, Houghton AK, Jones PS, McArthur D, Montgomery B, Ratcliffe PD, Smith AR, Sutherland A, Weston MA, Wishart G. Palin R, et al. Among authors: mcarthur d. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6441-6. doi: 10.1016/j.bmcl.2009.09.028. Epub 2009 Sep 12. Bioorg Med Chem Lett. 2009. PMID: 19818611
Structure-activity studies of a novel series of isoxazole-3-carboxamide derivatives as TRPV1 antagonists.
Palin R, Abernethy L, Ansari N, Cameron K, Clarkson T, Dempster M, Dunn D, Easson AM, Edwards D, Maclean J, Everett K, Feilden H, Ho KK, Kultgen S, Littlewood P, McArthur D, McGregor D, McLuskey H, Neagu I, Neale S, Nisbet LA, Ohlmeyer M, Pham Q, Ratcliffe P, Rong Y, Roughton A, Sammons M, Swanson R, Tracey H, Walker G. Palin R, et al. Among authors: mcarthur d. Bioorg Med Chem Lett. 2011 Feb 1;21(3):892-8. doi: 10.1016/j.bmcl.2010.12.092. Epub 2010 Dec 23. Bioorg Med Chem Lett. 2011. PMID: 21236666
Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists.
Kiyoi T, Adam JM, Clark JK, Davies K, Easson AM, Edwards D, Feilden H, Fields R, Francis S, Jeremiah F, McArthur D, Morrison AJ, Prosser A, Ratcliffe PD, Schulz J, Wishart G, Baker J, Campbell R, Cottney JE, Deehan M, Epemolu O, Evans L. Kiyoi T, et al. Among authors: mcarthur d. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1748-53. doi: 10.1016/j.bmcl.2011.01.082. Epub 2011 Jan 22. Bioorg Med Chem Lett. 2011. PMID: 21316962
Identification of potent, soluble, and orally active TRPV1 antagonists.
Ratcliffe P, Maclean J, Abernethy L, Clarkson T, Dempster M, Easson AM, Edwards D, Everett K, Feilden H, Littlewood P, McArthur D, McGregor D, McLuskey H, Nimz O, Nisbet LA, Palin R, Tracey H, Walker G. Ratcliffe P, et al. Among authors: mcarthur d. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2559-63. doi: 10.1016/j.bmcl.2011.01.112. Epub 2011 Jan 31. Bioorg Med Chem Lett. 2011. PMID: 21435873
Discovery of potent, soluble and orally active TRPV1 antagonists. Structure-activity relationships of a series of isoxazoles.
Ratcliffe P, Abernethy L, Ansari N, Cameron K, Clarkson T, Dempster M, Dunn D, Easson AM, Edwards D, Everett K, Feilden H, Ho KK, Kultgen S, Littlewood P, Maclean J, McArthur D, McGregor D, McLuskey H, Neagu I, Nimz O, Nisbet LA, Ohlmeyer M, Palin R, Pham Q, Rong Y, Roughton A, Sammons M, Swanson R, Tracey H, Walker G. Ratcliffe P, et al. Among authors: mcarthur d. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4652-7. doi: 10.1016/j.bmcl.2011.01.051. Epub 2011 Jan 26. Bioorg Med Chem Lett. 2011. PMID: 21723725
Stabilization of the RAS:PDE6D Complex Is a Novel Strategy to Inhibit RAS Signaling.
Yelland T, Garcia E, Parry C, Kowalczyk D, Wojnowska M, Gohlke A, Zalar M, Cameron K, Goodwin G, Yu Q, Zhu PC, ElMaghloob Y, Pugliese A, Archibald L, Jamieson A, Chen YX, McArthur D, Bower J, Ismail S. Yelland T, et al. Among authors: mcarthur d. J Med Chem. 2022 Feb 10;65(3):1898-1914. doi: 10.1021/acs.jmedchem.1c01265. Epub 2022 Feb 1. J Med Chem. 2022. PMID: 35104933 Free PMC article.
A Novel Small-Molecule Inhibitor of MRCK Prevents Radiation-Driven Invasion in Glioblastoma.
Birch JL, Strathdee K, Gilmour L, Vallatos A, McDonald L, Kouzeli A, Vasan R, Qaisi AH, Croft DR, Crighton D, Gill K, Gray CH, Konczal J, Mezna M, McArthur D, Schüttelkopf AW, McConnell P, Sime M, Holmes WM, Bower J, McKinnon HJ, Drysdale M, Olson MF, Chalmers AJ. Birch JL, et al. Among authors: mcarthur d. Cancer Res. 2018 Nov 15;78(22):6509-6522. doi: 10.1158/0008-5472.CAN-18-1697. Epub 2018 Oct 2. Cancer Res. 2018. PMID: 30279244
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. Unbekandt M, et al. Among authors: mcarthur d. Cancer Res. 2018 Apr 15;78(8):2096-2114. doi: 10.1158/0008-5472.CAN-17-2870. Epub 2018 Jan 30. Cancer Res. 2018. PMID: 29382705 Free PMC article.
339 results