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AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models.
Weir HM, Bradbury RH, Lawson M, Rabow AA, Buttar D, Callis RJ, Curwen JO, de Almeida C, Ballard P, Hulse M, Donald CS, Feron LJ, Karoutchi G, MacFaul P, Moss T, Norman RA, Pearson SE, Tonge M, Davies G, Walker GE, Wilson Z, Rowlinson R, Powell S, Sadler C, Richmond G, Ladd B, Pazolli E, Mazzola AM, D'Cruz C, De Savi C. Weir HM, et al. Among authors: karoutchi g. Cancer Res. 2016 Jun 1;76(11):3307-18. doi: 10.1158/0008-5472.CAN-15-2357. Epub 2016 Mar 28. Cancer Res. 2016. PMID: 27020862
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.
De Savi C, Bradbury RH, Rabow AA, Norman RA, de Almeida C, Andrews DM, Ballard P, Buttar D, Callis RJ, Currie GS, Curwen JO, Davies CD, Donald CS, Feron LJ, Gingell H, Glossop SC, Hayter BR, Hussain S, Karoutchi G, Lamont SG, MacFaul P, Moss TA, Pearson SE, Tonge M, Walker GE, Weir HM, Wilson Z. De Savi C, et al. Among authors: karoutchi g. J Med Chem. 2015 Oct 22;58(20):8128-40. doi: 10.1021/acs.jmedchem.5b00984. Epub 2015 Oct 7. J Med Chem. 2015. PMID: 26407012
Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode.
Finlay MR, Acton DG, Andrews DM, Barker AJ, Dennis M, Fisher E, Graham MA, Green CP, Heaton DW, Karoutchi G, Loddick SA, Morgentin R, Roberts A, Tucker JA, Weir HM. Finlay MR, et al. Among authors: karoutchi g. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4442-6. doi: 10.1016/j.bmcl.2008.06.027. Epub 2008 Jun 12. Bioorg Med Chem Lett. 2008. PMID: 18617397
Selective non zinc binding inhibitors of MMP13.
De Savi C, Morley AD, Ting A, Nash I, Karabelas K, Wood CM, James M, Norris SJ, Karoutchi G, Rankine N, Hamlin G, Macfaul PA, Ryan D, Baker SV, Hargreaves D, Gerhardt S. De Savi C, et al. Among authors: karoutchi g. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4215-9. doi: 10.1016/j.bmcl.2011.05.075. Epub 2011 May 27. Bioorg Med Chem Lett. 2011. PMID: 21669521
Dipeptidyl nitrile inhibitors of Cathepsin L.
Asaad N, Bethel PA, Coulson MD, Dawson JE, Ford SJ, Gerhardt S, Grist M, Hamlin GA, James MJ, Jones EV, Karoutchi GI, Kenny PW, Morley AD, Oldham K, Rankine N, Ryan D, Wells SL, Wood L, Augustin M, Krapp S, Simader H, Steinbacher S. Asaad N, et al. Among authors: karoutchi gi. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4280-3. doi: 10.1016/j.bmcl.2009.05.071. Epub 2009 May 27. Bioorg Med Chem Lett. 2009. PMID: 19515558
Design of selective Cathepsin inhibitors.
Bethel PA, Gerhardt S, Jones EV, Kenny PW, Karoutchi GI, Morley AD, Oldham K, Rankine N, Augustin M, Krapp S, Simader H, Steinbacher S. Bethel PA, et al. Among authors: karoutchi gi. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4622-5. doi: 10.1016/j.bmcl.2009.06.090. Epub 2009 Jun 27. Bioorg Med Chem Lett. 2009. PMID: 19616430