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Page 1
Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.
Fidanze SD, Liu D, Mantei RA, Hasvold LA, Pratt JK, Sheppard GS, Wang L, Holms JH, Dai Y, Aguirre A, Bogdan A, Dietrich JD, Marjanovic J, Park CH, Hutchins CW, Lin X, Bui MH, Huang X, Wilcox D, Li L, Wang R, Kovar P, Magoc TJ, Rajaraman G, Albert DH, Shen Y, Kati WM, McDaniel KF. Fidanze SD, et al. Among authors: sheppard gs. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1804-1810. doi: 10.1016/j.bmcl.2018.04.020. Epub 2018 Apr 11. Bioorg Med Chem Lett. 2018. PMID: 29678460
Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.
Wang GT, Mantei RA, Hubbard RD, Wilsbacher JL, Zhang Q, Tucker L, Hu X, Kovar P, Johnson EF, Osterling DJ, Bouska J, Wang J, Davidsen SK, Bell RL, Sheppard GS. Wang GT, et al. Among authors: sheppard gs. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6067-71. doi: 10.1016/j.bmcl.2010.08.052. Epub 2010 Aug 13. Bioorg Med Chem Lett. 2010. PMID: 20817523
Methylpyrrole inhibitors of BET bromodomains.
Hasvold LA, Sheppard GS, Wang L, Fidanze SD, Liu D, Pratt JK, Mantei RA, Wada CK, Hubbard R, Shen Y, Lin X, Huang X, Warder SE, Wilcox D, Li L, Buchanan FG, Smithee L, Albert DH, Magoc TJ, Park CH, Petros AM, Panchal SC, Sun C, Kovar P, Soni NB, Elmore SW, Kati WM, McDaniel KF. Hasvold LA, et al. Among authors: sheppard gs. Bioorg Med Chem Lett. 2017 May 15;27(10):2225-2233. doi: 10.1016/j.bmcl.2017.02.057. Epub 2017 Feb 24. Bioorg Med Chem Lett. 2017. PMID: 28268136
Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.
Wang L, Pratt JK, Soltwedel T, Sheppard GS, Fidanze SD, Liu D, Hasvold LA, Mantei RA, Holms JH, McClellan WJ, Wendt MD, Wada C, Frey R, Hansen TM, Hubbard R, Park CH, Li L, Magoc TJ, Albert DH, Lin X, Warder SE, Kovar P, Huang X, Wilcox D, Wang R, Rajaraman G, Petros AM, Hutchins CW, Panchal SC, Sun C, Elmore SW, Shen Y, Kati WM, McDaniel KF. Wang L, et al. Among authors: sheppard gs. J Med Chem. 2017 May 11;60(9):3828-3850. doi: 10.1021/acs.jmedchem.7b00017. Epub 2017 Apr 21. J Med Chem. 2017. PMID: 28368119
Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies.
Bui MH, Lin X, Albert DH, Li L, Lam LT, Faivre EJ, Warder SE, Huang X, Wilcox D, Donawho CK, Sheppard GS, Wang L, Fidanze S, Pratt JK, Liu D, Hasvold L, Uziel T, Lu X, Kohlhapp F, Fang G, Elmore SW, Rosenberg SH, McDaniel KF, Kati WM, Shen Y. Bui MH, et al. Among authors: sheppard gs. Cancer Res. 2017 Jun 1;77(11):2976-2989. doi: 10.1158/0008-5472.CAN-16-1793. Epub 2017 Apr 17. Cancer Res. 2017. PMID: 28416490
Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
McDaniel KF, Wang L, Soltwedel T, Fidanze SD, Hasvold LA, Liu D, Mantei RA, Pratt JK, Sheppard GS, Bui MH, Faivre EJ, Huang X, Li L, Lin X, Wang R, Warder SE, Wilcox D, Albert DH, Magoc TJ, Rajaraman G, Park CH, Hutchins CW, Shen JJ, Edalji RP, Sun CC, Martin R, Gao W, Wong S, Fang G, Elmore SW, Shen Y, Kati WM. McDaniel KF, et al. Among authors: sheppard gs. J Med Chem. 2017 Oct 26;60(20):8369-8384. doi: 10.1021/acs.jmedchem.7b00746. Epub 2017 Oct 12. J Med Chem. 2017. PMID: 28949521
Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer.
Faivre EJ, McDaniel KF, Albert DH, Mantena SR, Plotnik JP, Wilcox D, Zhang L, Bui MH, Sheppard GS, Wang L, Sehgal V, Lin X, Huang X, Lu X, Uziel T, Hessler P, Lam LT, Bellin RJ, Mehta G, Fidanze S, Pratt JK, Liu D, Hasvold LA, Sun C, Panchal SC, Nicolette JJ, Fossey SL, Park CH, Longenecker K, Bigelow L, Torrent M, Rosenberg SH, Kati WM, Shen Y. Faivre EJ, et al. Among authors: sheppard gs. Nature. 2020 Feb;578(7794):306-310. doi: 10.1038/s41586-020-1930-8. Epub 2020 Jan 22. Nature. 2020. PMID: 31969702
Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain.
Sheppard GS, Wang L, Fidanze SD, Hasvold LA, Liu D, Pratt JK, Park CH, Longenecker K, Qiu W, Torrent M, Kovar PJ, Bui M, Faivre E, Huang X, Lin X, Wilcox D, Zhang L, Shen Y, Albert DH, Magoc TJ, Rajaraman G, Kati WM, McDaniel KF. Sheppard GS, et al. J Med Chem. 2020 May 28;63(10):5585-5623. doi: 10.1021/acs.jmedchem.0c00628. Epub 2020 May 7. J Med Chem. 2020. PMID: 32324999
Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.
Sheppard GS, Wang J, Kawai M, Fidanze SD, BaMaung NY, Erickson SA, Barnes DM, Tedrow JS, Kolaczkowski L, Vasudevan A, Park DC, Wang GT, Sanders WJ, Mantei RA, Palazzo F, Tucker-Garcia L, Lou P, Zhang Q, Park CH, Kim KH, Petros A, Olejniczak E, Nettesheim D, Hajduk P, Henkin J, Lesniewski R, Davidsen SK, Bell RL. Sheppard GS, et al. J Med Chem. 2006 Jun 29;49(13):3832-49. doi: 10.1021/jm0601001. J Med Chem. 2006. PMID: 16789740
Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids.
Wang GT, Mantei RA, Kawai M, Tedrow JS, Barnes DM, Wang J, Zhang Q, Lou P, Garcia LA, Bouska J, Yates M, Park C, Judge RA, Lesniewski R, Sheppard GS, Bell RL. Wang GT, et al. Among authors: sheppard gs. Bioorg Med Chem Lett. 2007 May 15;17(10):2817-22. doi: 10.1016/j.bmcl.2007.02.062. Epub 2007 Feb 25. Bioorg Med Chem Lett. 2007. PMID: 17350258
37 results