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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: rzasa rm. J Med Chem. 2008 Oct 23;51(20):6271-9. doi: 10.1021/jm8005417. Epub 2008 Sep 26. J Med Chem. 2008. PMID: 18817365
Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.
Doherty EM, Fotsch C, Bannon AW, Bo Y, Chen N, Dominguez C, Falsey J, Gavva NR, Katon J, Nixey T, Ognyanov VI, Pettus L, Rzasa RM, Stec M, Surapaneni S, Tamir R, Zhu J, Treanor JJ, Norman MH. Doherty EM, et al. Among authors: rzasa rm. J Med Chem. 2007 Jul 26;50(15):3515-27. doi: 10.1021/jm070190p. Epub 2007 Jun 22. J Med Chem. 2007. PMID: 17585750
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.
Rzasa RM, Frohn MJ, Andrews KL, Chmait S, Chen N, Clarine JG, Davis C, Eastwood HA, Horne DB, Hu E, Jones AD, Kaller MR, Kunz RK, Miller S, Monenschein H, Nguyen T, Pickrell AJ, Porter A, Reichelt A, Zhao X, Treanor JJS, Allen JR. Rzasa RM, et al. Bioorg Med Chem. 2014 Dec 1;22(23):6570-6585. doi: 10.1016/j.bmc.2014.10.013. Bioorg Med Chem. 2014. PMID: 25456383
Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease.
Cushing TD, Hao X, Shin Y, Andrews K, Brown M, Cardozo M, Chen Y, Duquette J, Fisher B, Gonzalez-Lopez de Turiso F, He X, Henne KR, Hu YL, Hungate R, Johnson MG, Kelly RC, Lucas B, McCarter JD, McGee LR, Medina JC, San Miguel T, Mohn D, Pattaropong V, Pettus LH, Reichelt A, Rzasa RM, Seganish J, Tasker AS, Wahl RC, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang D, Metz DP. Cushing TD, et al. Among authors: rzasa rm. J Med Chem. 2015 Jan 8;58(1):480-511. doi: 10.1021/jm501624r. Epub 2014 Dec 3. J Med Chem. 2015. PMID: 25469863
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: rzasa rm. 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 and synthesis of 6-oxo-1,6-dihydropyridines as CDK5 inhibitors.
Kaller MR, Zhong W, Henley C, Magal E, Nguyen T, Powers D, Rzasa RM, Wang W, Xiong X, Norman MH. Kaller MR, et al. Among authors: rzasa rm. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6591-4. doi: 10.1016/j.bmcl.2009.10.027. Epub 2009 Oct 13. Bioorg Med Chem Lett. 2009. PMID: 19864130
Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors.
Zhong W, Liu H, Kaller MR, Henley C, Magal E, Nguyen T, Osslund TD, Powers D, Rzasa RM, Wang HL, Wang W, Xiong X, Zhang J, Norman MH. Zhong W, et al. Among authors: rzasa rm. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5384-9. doi: 10.1016/j.bmcl.2007.07.045. Epub 2007 Aug 6. Bioorg Med Chem Lett. 2007. PMID: 17709247
16 results