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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: wang l, wang r. 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
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: wang r. 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
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: wang l, wang r. 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
Structure-activity relationships for a novel series of thiazolyl phenyl ether derivatives exhibiting potent and selective acetyl-CoA carboxylase 2 inhibitory activity.
Clark RF, Zhang T, Xin Z, Liu G, Wang Y, Hansen TM, Wang X, Wang R, Zhang X, Frevert EU, Camp HS, Beutel BA, Sham HL, Gu YG. Clark RF, et al. Among authors: wang x, wang y, wang r. Bioorg Med Chem Lett. 2006 Dec 1;16(23):6078-81. doi: 10.1016/j.bmcl.2006.08.100. Epub 2006 Sep 14. Bioorg Med Chem Lett. 2006. PMID: 16973360
The synthesis and structure-activity relationship studies of selective acetyl-CoA carboxylase inhibitors containing 4-(thiazol-5-yl)but-3-yn-2-amino motif: polar region modifications.
Xu X, Weitzberg M, Keyes RF, Li Q, Wang R, Wang X, Zhang X, Frevert EU, Camp HS, Beutel BA, Sham HL, Gu YG. Xu X, et al. Among authors: wang x, wang r. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1803-7. doi: 10.1016/j.bmcl.2006.12.047. Epub 2006 Dec 21. Bioorg Med Chem Lett. 2007. PMID: 17234407
Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1- methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors.
Gu YG, Weitzberg M, Clark RF, Xu X, Li Q, Zhang T, Hansen TM, Liu G, Xin Z, Wang X, Wang R, McNally T, Zinker BA, Frevert EU, Camp HS, Beutel BA, Sham HL. Gu YG, et al. Among authors: wang x, wang r. J Med Chem. 2006 Jun 29;49(13):3770-3. doi: 10.1021/jm060484v. J Med Chem. 2006. PMID: 16789734
N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as acetyl-coA carboxylase inhibitors--improvement of cardiovascular and neurological liabilities via structural modifications.
Gu YG, Weitzberg M, Clark RF, Xu X, Li Q, Lubbers NL, Yang Y, Beno DW, Widomski DL, Zhang T, Hansen TM, Keyes RF, Waring JF, Carroll SL, Wang X, Wang R, Healan-Greenberg CH, Blomme EA, Beutel BA, Sham HL, Camp HS. Gu YG, et al. Among authors: wang x, wang r. J Med Chem. 2007 Mar 8;50(5):1078-82. doi: 10.1021/jm070035a. Epub 2007 Feb 14. J Med Chem. 2007. PMID: 17298049
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