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Page 1
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.
Tria GS, Abrams T, Baird J, Burks HE, Firestone B, Gaither LA, Hamann LG, He G, Kirby CA, Kim S, Lombardo F, Macchi KJ, McDonnell DP, Mishina Y, Norris JD, Nunez J, Springer C, Sun Y, Thomsen NM, Wang C, Wang J, Yu B, Tiong-Yip CL, Peukert S. Tria GS, et al. Among authors: sun y. J Med Chem. 2018 Apr 12;61(7):2837-2864. doi: 10.1021/acs.jmedchem.7b01682. Epub 2018 Mar 22. J Med Chem. 2018. PMID: 29562737
Design and structure-activity relationships of potent and selective inhibitors of undecaprenyl pyrophosphate synthase (UPPS): tetramic, tetronic acids and dihydropyridin-2-ones.
Peukert S, Sun Y, Zhang R, Hurley B, Sabio M, Shen X, Gray C, Dzink-Fox J, Tao J, Cebula R, Wattanasin S. Peukert S, et al. Among authors: sun y. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1840-4. doi: 10.1016/j.bmcl.2008.02.009. Epub 2008 Feb 10. Bioorg Med Chem Lett. 2008. PMID: 18295483
1-amino-4-benzylphthalazines as orally bioavailable smoothened antagonists with antitumor activity.
Miller-Moslin K, Peukert S, Jain RK, McEwan MA, Karki R, Llamas L, Yusuff N, He F, Li Y, Sun Y, Dai M, Perez L, Michael W, Sheng T, Lei H, Zhang R, Williams J, Bourret A, Ramamurthy A, Yuan J, Guo R, Matsumoto M, Vattay A, Maniara W, Amaral A, Dorsch M, Kelleher JF 3rd. Miller-Moslin K, et al. Among authors: sun y. J Med Chem. 2009 Jul 9;52(13):3954-68. doi: 10.1021/jm900309j. J Med Chem. 2009. PMID: 19469545
Discovery of NVP-LEQ506, a second-generation inhibitor of smoothened.
Peukert S, He F, Dai M, Zhang R, Sun Y, Miller-Moslin K, McEwan M, Lagu B, Wang K, Yusuff N, Bourret A, Ramamurthy A, Maniara W, Amaral A, Vattay A, Wang A, Guo R, Yuan J, Green J, Williams J, Buonamici S, Kelleher JF 3rd, Dorsch M. Peukert S, et al. Among authors: sun y. ChemMedChem. 2013 Aug;8(8):1261-5. doi: 10.1002/cmdc.201300217. Epub 2013 Jul 2. ChemMedChem. 2013. PMID: 23821351 No abstract available.
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.
Burks HE, Abrams T, Kirby CA, Baird J, Fekete A, Hamann LG, Kim S, Lombardo F, Loo A, Lubicka D, Macchi K, McDonnell DP, Mishina Y, Norris JD, Nunez J, Saran C, Sun Y, Thomsen NM, Wang C, Wang J, Peukert S. Burks HE, et al. Among authors: sun y. J Med Chem. 2017 Apr 13;60(7):2790-2818. doi: 10.1021/acs.jmedchem.6b01468. Epub 2017 Mar 15. J Med Chem. 2017. PMID: 28296398
Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders.
Bonazzi S, Goold CP, Gray A, Thomsen NM, Nunez J, Karki RG, Gorde A, Biag JD, Malik HA, Sun Y, Liang G, Lubicka D, Salas S, Labbe-Giguere N, Keaney EP, McTighe S, Liu S, Deng L, Piizzi G, Lombardo F, Burdette D, Dodart JC, Wilson CJ, Peukert S, Curtis D, Hamann LG, Murphy LO. Bonazzi S, et al. Among authors: sun y. J Med Chem. 2020 Feb 13;63(3):1068-1083. doi: 10.1021/acs.jmedchem.9b01398. Epub 2020 Jan 31. J Med Chem. 2020. PMID: 31955578
Identification of Brain-Penetrant ATP-Competitive mTOR Inhibitors for CNS Syndromes.
Bonazzi S, Gray A, Thomsen NM, Biag J, Labbe-Giguere N, Keaney EP, Malik HA, Sun Y, Nunez J, Karki RG, Knapp M, Elling R, Fuller J, Pardee G, Craig L, Capre K, Salas S, Gorde A, Liang G, Lubicka D, McTighe SM, Goold C, Liu S, Deng L, Hong J, Fekete A, Stadelmann P, Frieauff W, Elhajouji A, Bauer D, Lerchner A, Radetich B, Furet P, Piizzi G, Burdette D, Wilson CJ, Peukert S, Hamann LG, Murphy LO, Curtis D. Bonazzi S, et al. Among authors: sun y. J Med Chem. 2023 Jul 13;66(13):9095-9119. doi: 10.1021/acs.jmedchem.3c00705. Epub 2023 Jul 3. J Med Chem. 2023. PMID: 37399505
Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.
Mulvihill MJ, Ji QS, Coate HR, Cooke A, Dong H, Feng L, Foreman K, Rosenfeld-Franklin M, Honda A, Mak G, Mulvihill KM, Nigro AI, O'Connor M, Pirrit C, Steinig AG, Siu K, Stolz KM, Sun Y, Tavares PA, Yao Y, Gibson NW. Mulvihill MJ, et al. Among authors: sun y. Bioorg Med Chem. 2008 Feb 1;16(3):1359-75. doi: 10.1016/j.bmc.2007.10.061. Epub 2007 Oct 23. Bioorg Med Chem. 2008. PMID: 17983756
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