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The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure.
Cadilla R, Deaton DN, Do Y, Elkins PA, Ennulat D, Guss JH, Holt J, Jeune MR, King AG, Klapwijk JC, Kramer HF, Kramer NJ, Laffan SB, Masuria PI, McDougal AV, Mortenson PN, Musetti C, Peckham GE, Pietrak BL, Poole C, Price DJ, Rendina AR, Sati G, Saxty G, Shearer BG, Shewchuk LM, Sneddon HF, Stewart EL, Stuart JD, Thomas DN, Thomson SA, Ward P, Wilson JW, Xu T, Youngman MA. Cadilla R, et al. Among authors: shewchuk lm. Bioorg Med Chem. 2020 Dec 1;28(23):115791. doi: 10.1016/j.bmc.2020.115791. Epub 2020 Oct 3. Bioorg Med Chem. 2020. PMID: 33059303
Potent dipeptide inhibitors of the pp60c-src SH2 domain.
Pacofsky GJ, Lackey K, Alligood KJ, Berman J, Charifson PS, Crosby RM, Dorsey GF Jr, Feldman PL, Gilmer TM, Hummel CW, Jordan SR, Mohr C, Shewchuk LM, Sternbach DD, Rodriguez M. Pacofsky GJ, et al. Among authors: shewchuk lm. J Med Chem. 1998 May 21;41(11):1894-908. doi: 10.1021/jm970853a. J Med Chem. 1998. PMID: 9599239
Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.
Bramson HN, Corona J, Davis ST, Dickerson SH, Edelstein M, Frye SV, Gampe RT Jr, Harris PA, Hassell A, Holmes WD, Hunter RN, Lackey KE, Lovejoy B, Luzzio MJ, Montana V, Rocque WJ, Rusnak D, Shewchuk L, Veal JM, Walker DH, Kuyper LF. Bramson HN, et al. J Med Chem. 2001 Dec 6;44(25):4339-58. doi: 10.1021/jm010117d. J Med Chem. 2001. PMID: 11728181
Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.
Catalano JG, Deaton DN, Furfine ES, Hassell AM, McFadyen RB, Miller AB, Miller LR, Shewchuk LM, Willard DH Jr, Wright LL. Catalano JG, et al. Among authors: shewchuk lm. Bioorg Med Chem Lett. 2004 Jan 5;14(1):275-8. doi: 10.1016/j.bmcl.2003.09.088. Bioorg Med Chem Lett. 2004. PMID: 14684342
Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.
Boros EE, Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Paulick MG, Shewchuk LM, Thompson JB, Willard DH Jr, Wright LL. Boros EE, et al. Among authors: shewchuk lm. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3425-9. doi: 10.1016/j.bmcl.2004.04.084. Bioorg Med Chem Lett. 2004. PMID: 15177446
Novel and potent cyclic cyanamide-based cathepsin K inhibitors.
Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Shewchuk LM, Tavares FX, Willard DH Jr, Wright LL. Deaton DN, et al. Among authors: shewchuk lm. Bioorg Med Chem Lett. 2005 Apr 1;15(7):1815-9. doi: 10.1016/j.bmcl.2005.02.033. Bioorg Med Chem Lett. 2005. PMID: 15780613
59 results