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Page 1
5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase.
Tarver JE, Jessop TC, Carlsen M, Augeri DJ, Fu Q, Healy JP, Heim-Riether A, Xu A, Taylor JA, Shen M, Keyes PE, David Kimball S, Yu XC, Miranda M, Liu Q, Swaffield JC, Nouraldeen A, Wilson AG, Finch R, Jhaver K, Foushee AM, Anderson S, Oravecz T, Carson KG. Tarver JE, et al. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6780-3. doi: 10.1016/j.bmcl.2009.09.082. Epub 2009 Sep 25. Bioorg Med Chem Lett. 2009. PMID: 19836229
Lead optimization and structure-based design of potent and bioavailable deoxycytidine kinase inhibitors.
Jessop TC, Tarver JE, Carlsen M, Xu A, Healy JP, Heim-Riether A, Fu Q, Taylor JA, Augeri DJ, Shen M, Stouch TR, Swanson RV, Tari LW, Hunter M, Hoffman I, Keyes PE, Yu XC, Miranda M, Liu Q, Swaffield JC, David Kimball S, Nouraldeen A, Wilson AG, Foushee AM, Jhaver K, Finch R, Anderson S, Oravecz T, Carson KG. Jessop TC, et al. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6784-7. doi: 10.1016/j.bmcl.2009.09.081. Epub 2009 Sep 25. Bioorg Med Chem Lett. 2009. PMID: 19836232
4H-Thieno[3,2-c]chromene based inhibitors of Notum Pectinacetylesterase.
Han Q, Pabba PK, Barbosa J, Mabon R, Healy JP, Gardyan MW, Terranova KM, Brommage R, Thompson AY, Schmidt JM, Wilson AG, Xu X, Tarver JE Jr, Carson KG. Han Q, et al. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1184-7. doi: 10.1016/j.bmcl.2016.01.038. Epub 2016 Jan 18. Bioorg Med Chem Lett. 2016. PMID: 26821819
Design, synthesis, and in vivo activity of novel inhibitors of delta-5 desaturase for the treatment of metabolic syndrome.
Baugh SD, Pabba PK, Barbosa J, Coulter E, Desai U, Gay JP, Gopinathan S, Han Q, Hari R, Kimball SD, Nguyen HV, Ni CY, Powell DR, Smith A, Terranova KM, Wilson A, Yu XC, Lombardo VK. Baugh SD, et al. Bioorg Med Chem Lett. 2015 Sep 15;25(18):3836-9. doi: 10.1016/j.bmcl.2015.07.066. Epub 2015 Jul 26. Bioorg Med Chem Lett. 2015. PMID: 26235947
Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restricted to the Intestinal Lumen, for the Treatment of Diabetes.
Goodwin NC, Ding ZM, Harrison BA, Strobel ED, Harris AL, Smith M, Thompson AY, Xiong W, Mseeh F, Bruce DJ, Diaz D, Gopinathan S, Li L, O'Neill E, Thiel M, Wilson AG, Carson KG, Powell DR, Rawlins DB. Goodwin NC, et al. J Med Chem. 2017 Jan 26;60(2):710-721. doi: 10.1021/acs.jmedchem.6b01541. Epub 2017 Jan 17. J Med Chem. 2017. PMID: 28045524
Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma.
Harrison BA, Whitlock NA, Voronkov MV, Almstead ZY, Gu KJ, Mabon R, Gardyan M, Hamman BD, Allen J, Gopinathan S, McKnight B, Crist M, Zhang Y, Liu Y, Courtney LF, Key B, Zhou J, Patel N, Yates PW, Liu Q, Wilson AG, Kimball SD, Crosson CE, Rice DS, Rawlins DB. Harrison BA, et al. J Med Chem. 2009 Nov 12;52(21):6515-8. doi: 10.1021/jm901226j. J Med Chem. 2009. PMID: 19831390
Inhibition of sphingosine-1-phosphate lyase for the treatment of autoimmune disorders.
Bagdanoff JT, Donoviel MS, Nouraldeen A, Tarver J, Fu Q, Carlsen M, Jessop TC, Zhang H, Hazelwood J, Nguyen H, Baugh SD, Gardyan M, Terranova KM, Barbosa J, Yan J, Bednarz M, Layek S, Courtney LF, Taylor J, Digeorge-Foushee AM, Gopinathan S, Bruce D, Smith T, Moran L, O'Neill E, Kramer J, Lai Z, Kimball SD, Liu Q, Sun W, Yu S, Swaffield J, Wilson A, Main A, Carson KG, Oravecz T, Augeri DJ. Bagdanoff JT, et al. J Med Chem. 2009 Jul 9;52(13):3941-53. doi: 10.1021/jm900278w. J Med Chem. 2009. PMID: 19489538
Inhibition of sphingosine 1-phosphate lyase for the treatment of rheumatoid arthritis: discovery of (E)-1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone oxime (LX2931) and (1R,2S,3R)-1-(2-(isoxazol-3-yl)-1H-imidazol-4-yl)butane-1,2,3,4-tetraol (LX2932).
Bagdanoff JT, Donoviel MS, Nouraldeen A, Carlsen M, Jessop TC, Tarver J, Aleem S, Dong L, Zhang H, Boteju L, Hazelwood J, Yan J, Bednarz M, Layek S, Owusu IB, Gopinathan S, Moran L, Lai Z, Kramer J, Kimball SD, Yalamanchili P, Heydorn WE, Frazier KS, Brooks B, Brown P, Wilson A, Sonnenburg WK, Main A, Carson KG, Oravecz T, Augeri DJ. Bagdanoff JT, et al. J Med Chem. 2010 Dec 23;53(24):8650-62. doi: 10.1021/jm101183p. Epub 2010 Nov 22. J Med Chem. 2010. PMID: 21090716 Clinical Trial.
42 results