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Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).
Rai G, Brimacombe KR, Mott BT, Urban DJ, Hu X, Yang SM, Lee TD, Cheff DM, Kouznetsova J, Benavides GA, Pohida K, Kuenstner EJ, Luci DK, Lukacs CM, Davies DR, Dranow DM, Zhu H, Sulikowski G, Moore WJ, Stott GM, Flint AJ, Hall MD, Darley-Usmar VM, Neckers LM, Dang CV, Waterson AG, Simeonov A, Jadhav A, Maloney DJ. Rai G, et al. Among authors: brimacombe kr. J Med Chem. 2017 Nov 22;60(22):9184-9204. doi: 10.1021/acs.jmedchem.7b00941. Epub 2017 Nov 9. J Med Chem. 2017. PMID: 29120638 Free PMC article.
Collateral sensitivity of multidrug-resistant cells to the orphan drug tiopronin.
Goldsborough AS, Handley MD, Dulcey AE, Pluchino KM, Kannan P, Brimacombe KR, Hall MD, Griffiths G, Gottesman MM. Goldsborough AS, et al. Among authors: brimacombe kr. J Med Chem. 2011 Jul 28;54(14):4987-97. doi: 10.1021/jm2001663. Epub 2011 Jun 24. J Med Chem. 2011. PMID: 21657271 Free PMC article. Retracted.
Synthesis and structure-activity evaluation of isatin-β-thiosemicarbazones with improved selective activity toward multidrug-resistant cells expressing P-glycoprotein.
Hall MD, Brimacombe KR, Varonka MS, Pluchino KM, Monda JK, Li J, Walsh MJ, Boxer MB, Warren TH, Fales HM, Gottesman MM. Hall MD, et al. Among authors: brimacombe kr. J Med Chem. 2011 Aug 25;54(16):5878-89. doi: 10.1021/jm2006047. Epub 2011 Aug 1. J Med Chem. 2011. PMID: 21721528 Free PMC article.
Structure-activity relationship studies and biological characterization of human NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors.
Duveau DY, Yasgar A, Wang Y, Hu X, Kouznetsova J, Brimacombe KR, Jadhav A, Simeonov A, Thomas CJ, Maloney DJ. Duveau DY, et al. Among authors: brimacombe kr. Bioorg Med Chem Lett. 2014 Jan 15;24(2):630-5. doi: 10.1016/j.bmcl.2013.11.081. Epub 2013 Dec 4. Bioorg Med Chem Lett. 2014. PMID: 24360556 Free PMC article.
Identification of ML251, a Potent Inhibitor of T. brucei and T. cruzi Phosphofructokinase.
Brimacombe KR, Walsh MJ, Liu L, Vásquez-Valdivieso MG, Morgan HP, McNae I, Fothergill-Gilmore LA, Michels PA, Auld DS, Simeonov A, Walkinshaw MD, Shen M, Boxer MB. Brimacombe KR, et al. ACS Med Chem Lett. 2013 Oct 30;5(1):12-7. doi: 10.1021/ml400259d. eCollection 2014 Jan 9. ACS Med Chem Lett. 2013. PMID: 24900769 Free PMC article.
106 results