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Discovery of Novel Aminotetralines and Aminochromanes as Selective and Competitive Glycine Transporter 1 (GlyT1) Inhibitors.
Amberg W, Lange UEW, Ochse M, Pohlki F, Behl B, Relo AL, Hornberger W, Hoft C, Mezler M, Sydor J, Wang Y, Zhao H, Brewer JT, Dietrich J, Li H, Akritopoulou-Zanze I, Lao Y, Hannick SM, Ku YY, Vasudevan A. Amberg W, et al. Among authors: zhao h. J Med Chem. 2018 Sep 13;61(17):7503-7524. doi: 10.1021/acs.jmedchem.8b00300. Epub 2018 Aug 27. J Med Chem. 2018. PMID: 30080045
De Novo Design, Synthesis, and Biological Evaluation of 3,4-Disubstituted Pyrrolidine Sulfonamides as Potent and Selective Glycine Transporter 1 Competitive Inhibitors.
Wang Y, Zhao H, Brewer JT, Li H, Lao Y, Amberg W, Behl B, Akritopoulou-Zanze I, Dietrich J, Lange UEW, Pohlki F, Hoft C, Hornberger W, Djuric SW, Sydor J, Mezler M, Relo AL, Vasudevan A. Wang Y, et al. Among authors: zhao h. J Med Chem. 2018 Sep 13;61(17):7486-7502. doi: 10.1021/acs.jmedchem.8b00295. Epub 2018 Jul 17. J Med Chem. 2018. PMID: 29969029
SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.
Curtin ML, Pliushchev MA, Li HQ, Torrent M, Dietrich JD, Jakob CG, Zhu H, Zhao H, Wang Y, Ji Z, Clark RF, Sarris KA, Selvaraju S, Shaw B, Algire MA, He Y, Richardson PL, Sweis RF, Sun C, Chiang GG, Michaelides MR. Curtin ML, et al. Among authors: zhao h. Bioorg Med Chem Lett. 2017 Apr 1;27(7):1576-1583. doi: 10.1016/j.bmcl.2017.02.030. Epub 2017 Feb 20. Bioorg Med Chem Lett. 2017. PMID: 28254486
Privileged scaffolds in lead generation.
Zhao H, Dietrich J. Zhao H, et al. Expert Opin Drug Discov. 2015 Jul;10(7):781-90. doi: 10.1517/17460441.2015.1041496. Epub 2015 May 10. Expert Opin Drug Discov. 2015. PMID: 25959748 Review.
Discovery and pharmacological evaluation of growth hormone secretagogue receptor antagonists.
Xin Z, Serby MD, Zhao H, Kosogof C, Szczepankiewicz BG, Liu M, Liu B, Hutchins CW, Sarris KA, Hoff ED, Falls HD, Lin CW, Ogiela CA, Collins CA, Brune ME, Bush EN, Droz BA, Fey TA, Knourek-Segel VE, Shapiro R, Jacobson PB, Beno DW, Turner TM, Sham HL, Liu G. Xin Z, et al. Among authors: zhao h. J Med Chem. 2006 Jul 27;49(15):4459-69. doi: 10.1021/jm060461g. J Med Chem. 2006. PMID: 16854051
Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors.
Xin Z, Zhao H, Serby MD, Liu B, Liu M, Szczepankiewicz BG, Nelson LT, Smith HT, Suhar TS, Janis RS, Cao N, Camp HS, Collins CA, Sham HL, Surowy TK, Liu G. Xin Z, et al. Among authors: zhao h. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4298-302. doi: 10.1016/j.bmcl.2008.06.088. Epub 2008 Jun 28. Bioorg Med Chem Lett. 2008. PMID: 18632269
Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.
Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ, Haasch DL, Wang S, Clampit JE, Johnson EF, Lubben TH, Stashko MA, Olejniczak ET, Sun C, Dorwin SA, Haskins K, Abad-Zapatero C, Fry EH, Hutchins CW, Sham HL, Rondinone CM, Trevillyan JM. Szczepankiewicz BG, et al. Among authors: zhao h. J Med Chem. 2006 Jun 15;49(12):3563-80. doi: 10.1021/jm060199b. J Med Chem. 2006. PMID: 16759099
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