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Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Boga SB, Alhassan AB, Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Zhu H, Desai J, Maloney K, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Cooper A, Kim RM, Kozlowski JA. Boga SB, et al. Among authors: kozlowski ja. Bioorg Med Chem Lett. 2017 Aug 15;27(16):3939-3943. doi: 10.1016/j.bmcl.2017.03.040. Epub 2017 Mar 18. Bioorg Med Chem Lett. 2017. PMID: 28720503
Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Babu Boga S, Alhassan AB, Yu W, Selyutin O, Yu Y, Anand R, Xu J, Kelly J, Duffy JL, Liu S, Yang C, Wu H, Cai J, Bennett C, Maloney KM, Tyagarajan S, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: kozlowski ja. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127390. doi: 10.1016/j.bmcl.2020.127390. Epub 2020 Jul 11. Bioorg Med Chem Lett. 2020. PMID: 32738973
Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Boga SB, Alhassan AB, Yu Y, Vaccaro H, Liu S, Yang C, Wu H, Cooper A, de Man J, Kaptein A, Maloney K, Hornak V, Gao YD, Fischmann TO, Raaijmakers H, Vu-Pham D, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: kozlowski ja. ACS Med Chem Lett. 2015 Dec 19;7(2):198-203. doi: 10.1021/acsmedchemlett.5b00463. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985298 Free PMC article.
Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity.
Yu W, Liu J, Clausen D, Yu Y, Duffy JL, Wang M, Xu S, Deng L, Suzuki T, Chung CC, Myers RW, Klein DJ, Fells JI, Holloway MK, Wu J, Wu G, Howell BJ, Barnard RJO, Kozlowski J. Yu W, et al. J Med Chem. 2021 Apr 22;64(8):4709-4729. doi: 10.1021/acs.jmedchem.0c02150. Epub 2021 Apr 2. J Med Chem. 2021. PMID: 33797924
Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2-Substituted Benzamide Zinc Binding Group.
Liu J, Yu Y, Kelly J, Sha D, Alhassan AB, Yu W, Maletic MM, Duffy JL, Klein DJ, Holloway MK, Carroll S, Howell BJ, Barnard RJO, Wolkenberg S, Kozlowski JA. Liu J, et al. Among authors: kozlowski ja. ACS Med Chem Lett. 2020 Oct 13;11(12):2476-2483. doi: 10.1021/acsmedchemlett.0c00462. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335670 Free PMC article.
Discovery of potent macrocyclic HCV NS5A inhibitors.
Yu W, Vibulbhan B, Rosenblum SB, Martin GS, Vellekoop AS, Holst CL, Coburn CA, Wong M, Selyutin O, Ji T, Zhong B, Hu B, Chen L, Dwyer MP, Jiang Y, Nair AG, Tong L, Zeng Q, Agrawal S, Carr D, Rokosz L, Liu R, Curry S, McMonagle P, Ingravallo P, Lahser F, Asante-Appiah E, Fells J, Kozlowski JA. Yu W, et al. Among authors: kozlowski ja. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3793-9. doi: 10.1016/j.bmcl.2016.05.042. Epub 2016 May 17. Bioorg Med Chem Lett. 2016. PMID: 27282743
I. Novel HCV NS5B polymerase inhibitors: discovery of indole 2-carboxylic acids with C3-heterocycles.
Anilkumar GN, Lesburg CA, Selyutin O, Rosenblum SB, Zeng Q, Jiang Y, Chan TY, Pu H, Vaccaro H, Wang L, Bennett F, Chen KX, Duca J, Gavalas S, Huang Y, Pinto P, Sannigrahi M, Velazquez F, Venkatraman S, Vibulbhan B, Agrawal S, Butkiewicz N, Feld B, Ferrari E, He Z, Jiang CK, Palermo RE, McMonagle P, Huang HC, Shih NY, Njoroge G, Kozlowski JA. Anilkumar GN, et al. Among authors: kozlowski ja. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5336-41. doi: 10.1016/j.bmcl.2011.07.021. Epub 2011 Jul 19. Bioorg Med Chem Lett. 2011. PMID: 21840715
Discovery of fused tricyclic core containing HCV NS5A inhibitors with pan-genotype activity.
Yu W, Coburn CA, Yang DY, Meinke PT, Wong M, Rosenblum SB, Chen KX, Njoroge GF, Chen L, Dwyer MP, Jiang Y, Nair AG, Selyutin O, Tong L, Zeng Q, Zhong B, Ji T, Hu B, Agrawal S, Xia E, Zhai Y, Liu R, Kong R, Ingravallo P, Asante-Appiah E, Nomeir A, Fells J, Kozlowski JA. Yu W, et al. Among authors: kozlowski ja. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3158-3162. doi: 10.1016/j.bmcl.2016.04.084. Epub 2016 Apr 30. Bioorg Med Chem Lett. 2016. PMID: 27180013
96 results