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Page 1
Synthesis of HDAC Inhibitor Libraries via Microscale Workflow.
Dykstra KD, Streckfuss E, Liu M, Liu J, Yu Y, Wang M, Kozlowski JA, Myers RW, Buevich AV, Maletic MM, Vachal P, Krska SW. Dykstra KD, et al. Among authors: yu y. ACS Med Chem Lett. 2021 Feb 8;12(3):337-342. doi: 10.1021/acsmedchemlett.0c00596. eCollection 2021 Mar 11. ACS Med Chem Lett. 2021. PMID: 33738059 Free PMC article.
Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties.
Xiao D, Zhu X, Yu Y, Shao N, Wu J, McCormick KD, Dhondi P, Qin J, Mazzola R, Tang H, Rao A, Siliphaivanh P, Qiu H, Yang X, Rivelli M, Garlisi CG, Eckel S, Mukhopadhyay G, Correll C, Rindgen D, Aslanian R, Palani A. Xiao D, et al. Among authors: yu y. Bioorg Med Chem Lett. 2014 Mar 15;24(6):1615-20. doi: 10.1016/j.bmcl.2014.01.043. Epub 2014 Feb 2. Bioorg Med Chem Lett. 2014. PMID: 24556380
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: yu w, yu y. 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 ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.
Yu W, Liu J, Yu Y, Zhang V, Clausen D, Kelly J, Wolkenberg S, Beshore D, Duffy JL, Chung CC, Myers RW, Klein DJ, Fells J, Holloway K, Wu J, Wu G, Howell BJ, Barnard RJO, Kozlowski J. Yu W, et al. Among authors: yu y. Bioorg Med Chem Lett. 2020 Jul 1;30(13):127197. doi: 10.1016/j.bmcl.2020.127197. Epub 2020 Apr 15. Bioorg Med Chem Lett. 2020. PMID: 32331932
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: yu y. 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
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.
Liu J, Kelly J, Yu W, Clausen D, Yu Y, Kim H, Duffy JL, Chung CC, Myers RW, Carroll S, Klein DJ, Fells J, Holloway MK, Wu J, Wu G, Howell BJ, Barnard RJO, Kozlowski JA. Liu J, et al. Among authors: yu w, yu y. ACS Med Chem Lett. 2020 Jun 22;11(7):1476-1483. doi: 10.1021/acsmedchemlett.0c00302. eCollection 2020 Jul 9. ACS Med Chem Lett. 2020. PMID: 32676157 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. Among authors: yu y. 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: yu w, yu y. 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 novel BTK inhibitors with carboxylic acids.
Gao X, Wang J, Liu J, Guiadeen D, Krikorian A, Boga SB, Alhassan AB, Selyutin O, Yu W, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Cooper A, Zhu H, Maloney K, Gao YD, Fischmann TO, 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. Gao X, et al. Among authors: yu w, yu y. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1471-1477. doi: 10.1016/j.bmcl.2016.11.079. Epub 2016 Nov 25. Bioorg Med Chem Lett. 2017. PMID: 28254166
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