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Page 1
Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.
Herberich B, Cao GQ, Chakrabarti PP, Falsey JR, Pettus L, Rzasa RM, Reed AB, Reichelt A, Sham K, Thaman M, Wurz RP, Xu S, Zhang D, Hsieh F, Lee MR, Syed R, Li V, Grosfeld D, Plant MH, Henkle B, Sherman L, Middleton S, Wong LM, Tasker AS. Herberich B, et al. Among authors: xu s. J Med Chem. 2008 Oct 23;51(20):6271-9. doi: 10.1021/jm8005417. Epub 2008 Sep 26. J Med Chem. 2008. PMID: 18817365
Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Wurz RP, Pettus LH, Xu S, Henkle B, Sherman L, Plant M, Miner K, McBride H, Wong LM, Saris CJ, Lee MR, Chmait S, Mohr C, Hsieh F, Tasker AS. Wurz RP, et al. Among authors: xu s. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4724-8. doi: 10.1016/j.bmcl.2009.06.058. Epub 2009 Jun 17. Bioorg Med Chem Lett. 2009. PMID: 19574047
3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Pettus LH, Xu S, Cao GQ, Chakrabarti PP, Rzasa RM, Sham K, Wurz RP, Zhang D, Middleton S, Henkle B, Plant MH, Saris CJ, Sherman L, Wong LM, Powers DA, Tudor Y, Yu V, Lee MR, Syed R, Hsieh F, Tasker AS. Pettus LH, et al. Among authors: xu s. J Med Chem. 2008 Oct 23;51(20):6280-92. doi: 10.1021/jm8005405. Epub 2008 Sep 26. J Med Chem. 2008. PMID: 18817364
Design, synthesis, and biological evaluation of potent c-Met inhibitors.
D'Angelo ND, Bellon SF, Booker SK, Cheng Y, Coxon A, Dominguez C, Fellows I, Hoffman D, Hungate R, Kaplan-Lefko P, Lee MR, Li C, Liu L, Rainbeau E, Reider PJ, Rex K, Siegmund A, Sun Y, Tasker AS, Xi N, Xu S, Yang Y, Zhang Y, Burgess TL, Dussault I, Kim TS. D'Angelo ND, et al. Among authors: xu s. J Med Chem. 2008 Sep 25;51(18):5766-79. doi: 10.1021/jm8006189. J Med Chem. 2008. PMID: 18763753
N-Aryl-gamma-lactams as integrin alphavbeta3 antagonists.
Xi N, Arvedson S, Eisenberg S, Han N, Handley M, Huang L, Huang Q, Kiselyov A, Liu Q, Lu Y, Nunez G, Osslund T, Powers D, Tasker AS, Wang L, Xiang T, Xu S, Zhang J, Zhu J, Kendall R, Dominguez C. Xi N, et al. Among authors: xu s. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2905-9. doi: 10.1016/j.bmcl.2004.03.033. Bioorg Med Chem Lett. 2004. PMID: 15125957
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.
Fotsch C, Han N, Arasasingham P, Bo Y, Carmouche M, Chen N, Davis J, Goldberg MH, Hale C, Hsieh FY, Kelly MG, Liu Q, Norman MH, Smith DM, Stec M, Tamayo N, Xi N, Xu S, Bannon AW, Baumgartner JW. Fotsch C, et al. Among authors: xu s. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1623-7. doi: 10.1016/j.bmcl.2005.01.060. Bioorg Med Chem Lett. 2005. PMID: 15745810
Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.
Pettus LH, Wurz RP, Xu S, Herberich B, Henkle B, Liu Q, McBride HJ, Mu S, Plant MH, Saris CJ, Sherman L, Wong LM, Chmait S, Lee MR, Mohr C, Hsieh F, Tasker AS. Pettus LH, et al. Among authors: xu s. J Med Chem. 2010 Apr 8;53(7):2973-85. doi: 10.1021/jm100095x. J Med Chem. 2010. PMID: 20218619
Discovery and optimization of a highly efficacious class of 5-aryl-2-aminopyridines as FMS-like tyrosine kinase 3 (FLT3) inhibitors.
Liu G, Abraham S, Liu X, Xu S, Rooks AM, Nepomuceno R, Dao A, Brigham D, Gitnick D, Insko DE, Gardner MF, Zarrinkar PP, Christopher R, Belli B, Armstrong RC, Holladay MW. Liu G, et al. Among authors: xu s. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3436-41. doi: 10.1016/j.bmcl.2015.07.023. Epub 2015 Jul 14. Bioorg Med Chem Lett. 2015. PMID: 26208887
Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index.
Liu G, Abraham S, Tran L, Vickers TD, Xu S, Hadd MJ, Quiambao S, Holladay MW, Hua H, Ford Pulido JM, Gunawardane RN, Davis MI, Eichelberger SR, Apuy JL, Gitnick D, Gardner MF, James J, Breider MA, Belli B, Armstrong RC, Treiber DK. Liu G, et al. Among authors: xu s. J Med Chem. 2012 Apr 12;55(7):3250-60. doi: 10.1021/jm201702g. Epub 2012 Mar 14. J Med Chem. 2012. PMID: 22380736
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