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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. Among authors: li c. 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
Identification of N-(1H-pyrazol-4-yl)carboxamide inhibitors of interleukin-1 receptor associated kinase 4: Bicyclic core modifications.
Lim J, Altman MD, Baker J, Brubaker JD, Chen H, Chen Y, Kleinschek MA, Li C, Liu D, Maclean JK, Mulrooney EF, Presland J, Rakhilina L, Smith GF, Yang R. Lim J, et al. Among authors: li c. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5384-8. doi: 10.1016/j.bmcl.2015.09.028. Epub 2015 Sep 11. Bioorg Med Chem Lett. 2015. PMID: 26403930
Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.
Northrup AB, Katcher MH, Altman MD, Chenard M, Daniels MH, Deshmukh SV, Falcone D, Guerin DJ, Hatch H, Li C, Lu W, Lutterbach B, Allison TJ, Patel SB, Reilly JF, Reutershan M, Rickert KW, Rosenstein C, Soisson SM, Szewczak AA, Walker D, Wilson K, Young JR, Pan BS, Dinsmore CJ. Northrup AB, et al. Among authors: li c. J Med Chem. 2013 Mar 28;56(6):2294-310. doi: 10.1021/jm301619u. Epub 2013 Mar 18. J Med Chem. 2013. PMID: 23379595
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Zhou H, McGowan MA, Lipford K, Christopher M, Fradera X, Witter D, Lesburg CA, Li C, Methot JL, Lampe J, Achab A, Shaffer L, Goldenblatt P, Shah S, Bass A, Schroeder G, Chen D, Zeng H, Augustin MA, Katz JD. Zhou H, et al. Among authors: li c. Bioorg Med Chem Lett. 2020 Jan 1;30(1):126715. doi: 10.1016/j.bmcl.2019.126715. Epub 2019 Oct 18. Bioorg Med Chem Lett. 2020. PMID: 31757666
Piperazinyl pyrimidine derivatives as potent gamma-secretase modulators.
Rivkin A, Ahearn SP, Chichetti SM, Kim YR, Li C, Rosenau A, Kattar SD, Jung J, Shah S, Hughes BL, Crispino JL, Middleton RE, Szewczak AA, Munoz B, Shearman MS. Rivkin A, et al. Among authors: li c. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1269-71. doi: 10.1016/j.bmcl.2009.11.101. Epub 2009 Nov 23. Bioorg Med Chem Lett. 2010. PMID: 20022243
Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3Kδ Immunomodulators.
Methot JL, Zhou H, McGowan MA, Anthony NJ, Christopher M, Garcia Y, Achab A, Lipford K, Trotter BW, Altman MD, Fradera X, Lesburg CA, Li C, Alves S, Chappell CP, Jain R, Mangado R, Pinheiro E, Williams SMG, Goldenblatt P, Hill A, Shaffer L, Chen D, Tong V, McLeod RL, Lee HH, Yu H, Shah S, Katz JD. Methot JL, et al. Among authors: li c. J Med Chem. 2021 Apr 22;64(8):5137-5156. doi: 10.1021/acs.jmedchem.1c00237. Epub 2021 Apr 2. J Med Chem. 2021. PMID: 33797901
Potent benzoazepinone γ-secretase modulators with improved bioavailability.
Methot JL, Fischer C, Li C, Rivkin A, Ahearn SP, Brown WC, Kattar S, Kelley E, Mampreian DM, Schell A, Rosenau A, Zhou H, Ball R, Deshmukh SV, Jeliazkova-Mecheva VV, Diaz D, Moy LY, Kenific CM, Moxham C, Shah S, Nuthall H, Szewczak AA, Hill A, Hughes B, Smotrov N, Munoz B, Miller TA, Shearman MS. Methot JL, et al. Among authors: li c. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3495-500. doi: 10.1016/j.bmcl.2015.06.032. Epub 2015 Jun 15. Bioorg Med Chem Lett. 2015. PMID: 26142947
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: li c. 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
Discovery of MK-4688: an Efficient Inhibitor of the HDM2-p53 Protein-Protein Interaction.
Reutershan MH, Machacek MR, Altman MD, Bogen S, Cai M, Cammarano C, Chen D, Christopher M, Cryan J, Daublain P, Fradera X, Geda P, Goldenblatt P, Hill AD, Kemper RA, Kutilek V, Li C, Martinez M, McCoy M, Nair L, Pan W, Thompson CF, Scapin G, Shizuka M, Spatz ML, Steinhuebel D, Sun B, Voss ME, Wang X, Yang L, Yeh TC, Dussault I, Marshall CG, Trotter BW. Reutershan MH, et al. Among authors: li c. J Med Chem. 2021 Nov 11;64(21):16213-16241. doi: 10.1021/acs.jmedchem.1c01524. Epub 2021 Oct 29. J Med Chem. 2021. PMID: 34714078
Lead optimization of 4,4-biaryl piperidine amides as γ-secretase inhibitors.
Close J, Heidebrecht R Jr, Hendrix J, Li C, Munoz B, Surdi L, Kattar S, Tempest P, Moses P, Geng X, Hughes B, Smotrov N, Moxham C, Chapnick J, Kariv I, Nikov G, Burke JE, Deshmukh S, Jeliazkova-Mecheva V, Leach JK, Diaz D, Xu L, Yang Z, Kwei G, Moy L, Shah S, Tanga F, Kenefic C, Savage D, Shearman M, Ball RG, McNevin MJ, Markarewicz A, Miller T. Close J, et al. Among authors: li c. Bioorg Med Chem Lett. 2012 May 1;22(9):3203-7. doi: 10.1016/j.bmcl.2012.03.038. Epub 2012 Mar 17. Bioorg Med Chem Lett. 2012. PMID: 22483609
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