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Structure Overhaul Affords a Potent Purine PI3Kδ Inhibitor with Improved Tolerability.
Methot JL, Zhou H, Kattar SD, McGowan MA, Wilson K, Garcia Y, Deng Y, Altman M, Fradera X, Lesburg C, Fischmann T, Li C, Alves S, Shah S, Fernandez R, Goldenblatt P, Hill A, Shaffer L, Chen D, Tong V, McLeod RL, Yu H, Bass A, Kemper R, Gatto NT, LaFranco-Scheuch L, Trotter BW, Guzi T, Katz JD. Methot JL, et al. Among authors: fischmann t. J Med Chem. 2019 May 9;62(9):4370-4382. doi: 10.1021/acs.jmedchem.8b01818. Epub 2019 Apr 22. J Med Chem. 2019. PMID: 30986068
Design, synthesis and SAR of thienopyridines as potent CHK1 inhibitors.
Zhao L, Zhang Y, Dai C, Guzi T, Wiswell D, Seghezzi W, Parry D, Fischmann T, Siddiqui MA. Zhao L, et al. Among authors: fischmann t. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7216-21. doi: 10.1016/j.bmcl.2010.10.105. Epub 2010 Oct 26. Bioorg Med Chem Lett. 2010. PMID: 21074424
Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.
Paruch K, Dwyer MP, Alvarez C, Brown C, Chan TY, Doll RJ, Keertikar K, Knutson C, McKittrick B, Rivera J, Rossman R, Tucker G, Fischmann T, Hruza A, Madison V, Nomeir AA, Wang Y, Kirschmeier P, Lees E, Parry D, Sgambellone N, Seghezzi W, Schultz L, Shanahan F, Wiswell D, Xu X, Zhou Q, James RA, Paradkar VM, Park H, Rokosz LR, Stauffer TM, Guzi TJ. Paruch K, et al. Among authors: fischmann t. ACS Med Chem Lett. 2010 May 17;1(5):204-8. doi: 10.1021/ml100051d. eCollection 2010 Aug 12. ACS Med Chem Lett. 2010. PMID: 24900195 Free PMC article.
Discovery of 5-Amino-N-(1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide Inhibitors of IRAK4.
Lim J, Altman MD, Baker J, Brubaker JD, Chen H, Chen Y, Fischmann T, Gibeau C, Kleinschek MA, Leccese E, Lesburg C, Maclean JK, Moy LY, Mulrooney EF, Presland J, Rakhilina L, Smith GF, Steinhuebel D, Yang R. Lim J, et al. Among authors: fischmann t. ACS Med Chem Lett. 2015 Apr 20;6(6):683-8. doi: 10.1021/acsmedchemlett.5b00107. eCollection 2015 Jun 11. ACS Med Chem Lett. 2015. PMID: 26101574 Free PMC article.
Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation.
Smith GF, Altman MD, Andresen B, Baker J, Brubaker JD, Chen H, Chen Y, Childers M, Donofrio A, Ferguson H, Fischer C, Fischmann TO, Gibeau C, Hicks A, Jin S, Kattar S, Kleinschek MA, Leccese E, Lesburg C, Li C, Lim J, Liu D, Maclean JKF, Mansoor F, Moy LY, Mulrooney EF, Necheva AS, Presland J, Rakhilina L, Yang R, Torres L, Zhang-Hoover J, Northrup A. Smith GF, et al. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2721-2726. doi: 10.1016/j.bmcl.2017.04.050. Epub 2017 Apr 18. Bioorg Med Chem Lett. 2017. PMID: 28501511
Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2.
Paruch K, Dwyer MP, Alvarez C, Brown C, Chan TY, Doll RJ, Keertikar K, Knutson C, McKittrick B, Rivera J, Rossman R, Tucker G, Fischmann TO, Hruza A, Madison V, Nomeir AA, Wang Y, Lees E, Parry D, Sgambellone N, Seghezzi W, Schultz L, Shanahan F, Wiswell D, Xu X, Zhou Q, James RA, Paradkar VM, Park H, Rokosz LR, Stauffer TM, Guzi TJ. Paruch K, et al. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6220-3. doi: 10.1016/j.bmcl.2007.09.017. Epub 2007 Sep 8. Bioorg Med Chem Lett. 2007. PMID: 17904841
68 results