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1.

Discovery of ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.

Yu, Wensheng; Liu, Jian; Yu, Younong; Zhang, Vivian; Clausen, Dane; Kelly, Joseph; Wolkenberg, Scott; Beshore, Douglas; Duffy, Joseph L; Chung, Christine C; Myers, Robert W; Klein, Daniel J; Fells, James; Holloway, Kate; Wu, Jin; Wu, Guoxin; Howell, Bonnie J; Barnard, Richard J O; Kozlowski, Joseph.

Bioorg Med Chem Lett ; 30(13): 127197, 2020 07 01.

Article in English | MEDLINE | ID: mdl-32331932

2.

Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.

Liu, Jian; Guiadeen, Deodial; Krikorian, Arto; Gao, Xiaolei; Wang, James; Babu Boga, Sobhana; Alhassan, Abdul-Basit; Yu, Wensheng; Selyutin, Oleg; Yu, Younong; Anand, Rajan; Xu, Jiayi; Kelly, Joseph; Duffy, Joseph L; Liu, Shilan; Yang, Chundao; Wu, Hao; Cai, Jiaqiang; Bennett, Chad; Maloney, Kevin M; Tyagarajan, Sriram; Gao, Ying-Duo; Fischmann, Thierry O; Presland, Jeremy; Mansueto, My; Xu, Zangwei; Leccese, Erica; Zhang-Hoover, Jie; Knemeyer, Ian; Garlisi, Charles G; Stivers, Peter; Brandish, Philip E; Hicks, Alexandra; Kim, Ronald; Kozlowski, Joseph A.

Bioorg Med Chem Lett ; 30(17): 127390, 2020 09 01.

Article in English | MEDLINE | ID: mdl-32738973

3.

Chemoselective Peptide Modification via Photocatalytic Tryptophan ß-Position Conjugation.

Yu, Younong; Zhang, Li-Kang; Buevich, Alexei V; Li, Guoqing; Tang, Haiqun; Vachal, Petr; Colletti, Steven L; Shi, Zhi-Cai.

J Am Chem Soc ; 140(22): 6797-6800, 2018 06 06.

Article in English | MEDLINE | ID: mdl-29762027

4.

Discovery of novel BTK inhibitors with carboxylic acids.

Gao, Xiaolei; Wang, James; Liu, Jian; Guiadeen, Deodial; Krikorian, Arto; Boga, Sobhana Babu; Alhassan, Abdul-Basit; Selyutin, Oleg; Yu, Wensheng; Yu, Younong; Anand, Rajan; Liu, Shilan; Yang, Chundao; Wu, Hao; Cai, Jiaqiang; Cooper, Alan; Zhu, Hugh; Maloney, Kevin; Gao, Ying-Duo; Fischmann, Thierry O; Presland, Jeremy; Mansueto, My; Xu, Zangwei; Leccese, Erica; Zhang-Hoover, Jie; Knemeyer, Ian; Garlisi, Charles G; Bays, Nathan; Stivers, Peter; Brandish, Philip E; Hicks, Alexandra; Kim, Ronald; Kozlowski, Joeseph A.

Bioorg Med Chem Lett ; 27(6): 1471-1477, 2017 03 15.

Article in English | MEDLINE | ID: mdl-28254166

5.

Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.

Boga, Sobhana Babu; Alhassan, Abdul-Basit; Liu, Jian; Guiadeen, Deodial; Krikorian, Arto; Gao, Xiaolei; Wang, James; Yu, Younong; Anand, Rajan; Liu, Shilan; Yang, Chundao; Wu, Hao; Cai, Jiaqiang; Zhu, Hugh; Desai, Jagdish; Maloney, Kevin; Gao, Ying-Duo; Fischmann, Thierry O; Presland, Jeremy; Mansueto, My; Xu, Zangwei; Leccese, Erica; Knemeyer, Ian; Garlisi, Charles G; Bays, Nathan; Stivers, Peter; Brandish, Philip E; Hicks, Alexandra; Cooper, Alan; Kim, Ronald M; Kozlowski, Joseph A.

Bioorg Med Chem Lett ; 27(16): 3939-3943, 2017 08 15.

Article in English | MEDLINE | ID: mdl-28720503

6.

Use of molecular modeling aided design to dial out hERG liability in adenosine A(2A) receptor antagonists.

Deng, Qiaolin; Lim, Yeon-Hee; Anand, Rajan; Yu, Younong; Kim, Jae-hun; Zhou, Wei; Zheng, Junying; Tempest, Paul; Levorse, Dorothy; Zhang, Xiaoping; Greene, Scott; Mullins, Deborra; Culberson, Chris; Sherborne, Brad; Parker, Eric M; Stamford, Andrew; Ali, Amjad.

Bioorg Med Chem Lett ; 25(15): 2958-62, 2015 Aug 01.

Article in English | MEDLINE | ID: mdl-26048804

7.

Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties.

Xiao, Dong; Zhu, Xiaohong; Yu, Younong; Shao, Ning; Wu, Jie; McCormick, Kevin D; Dhondi, Pawan; Qin, Jun; Mazzola, Robert; Tang, Haiqun; Rao, Ashwin; Siliphaivanh, Phieng; Qiu, Hongchen; Yang, Xiaoxin; Rivelli, Maria; Garlisi, Charles G; Eckel, Steve; Mukhopadhyay, Gitali; Correll, Craig; Rindgen, Diane; Aslanian, Robert; Palani, Anandan.

Bioorg Med Chem Lett ; 24(6): 1615-20, 2014 Mar 15.

Article in English | MEDLINE | ID: mdl-24556380

8.

Synthesis of HDAC Inhibitor Libraries via Microscale Workflow.

Dykstra, Kevin D; Streckfuss, Eric; Liu, Min; Liu, Jian; Yu, Younong; Wang, Ming; Kozlowski, Joseph A; Myers, Robert W; Buevich, Alexei V; Maletic, Milana M; Vachal, Petr; Krska, Shane W.

ACS Med Chem Lett ; 12(3): 337-342, 2021 Mar 11.

Article in English | MEDLINE | ID: mdl-33738059

9.

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, Wensheng; Liu, Jian; Clausen, Dane; Yu, Younong; Duffy, Joseph L; Wang, Ming; Xu, Shouning; Deng, Lin; Suzuki, Takao; Chung, Christine C; Myers, Robert W; Klein, Daniel J; Fells, James I; Holloway, M Katharine; Wu, Jin; Wu, Guoxin; Howell, Bonnie J; Barnard, Richard J O; Kozlowski, Joseph.

J Med Chem ; 64(8): 4709-4729, 2021 04 22.

Article in English | MEDLINE | ID: mdl-33797924

10.

Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2-Substituted Benzamide Zinc Binding Group.

Liu, Jian; Yu, Younong; Kelly, Joseph; Sha, Deyou; Alhassan, Abdul-Basit; Yu, Wensheng; Maletic, Milana M; Duffy, Joseph L; Klein, Daniel J; Holloway, M Katharine; Carroll, Steve; Howell, Bonnie J; Barnard, Richard J O; Wolkenberg, Scott; Kozlowski, Joseph A.

ACS Med Chem Lett ; 11(12): 2476-2483, 2020 Dec 10.

Article in English | MEDLINE | ID: mdl-33335670

11.

Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.

Liu, Jian; Kelly, Joseph; Yu, Wensheng; Clausen, Dane; Yu, Younong; Kim, Hyunjin; Duffy, Joseph L; Chung, Christine C; Myers, Robert W; Carroll, Steve; Klein, Daniel J; Fells, James; Holloway, M Katharine; Wu, Jin; Wu, Guoxin; Howell, Bonnie J; Barnard, Richard J O; Kozlowski, Joseph A.

ACS Med Chem Lett ; 11(7): 1476-1483, 2020 Jul 09.

Article in English | MEDLINE | ID: mdl-32676157

12.

3,4-Diamino-1,2,5-thiadiazole as potent and selective CXCR2 antagonists.

Biju, Purakkattle; Taveras, Arthur G; Yu, Younong; Zheng, Junying; Hipkin, R William; Fossetta, James; Fan, Xuedong; Fine, Jay; Lundell, Daniel.

Bioorg Med Chem Lett ; 19(5): 1434-7, 2009 Mar 01.

Article in English | MEDLINE | ID: mdl-19200721

13.

Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.

Biju, Purakkattle; Taveras, Arthur G; Dwyer, Michael P; Yu, Younong; Chao, Jianhua; Hipkin, R William; Fan, Xuedong; Rindgen, Diane; Fine, Jay; Lundell, Daniel.

Bioorg Med Chem Lett ; 19(5): 1431-3, 2009 Mar 01.

Article in English | MEDLINE | ID: mdl-19196511

14.

Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.

Aki, Cynthia; Chao, Jianping; Ferreira, Johan A; Dwyer, Michael P; Yu, Younong; Chao, Jianhua; Merritt, Robert J; Lai, Gaifa; Wu, Minglang; Hipkin, R William; Fan, Xuedong; Gonsiorek, Waldemar; Fosseta, James; Rindgen, Diane; Fine, Jay; Lundell, Daniel; Taveras, Arthur G; Biju, Purakkattle.

Bioorg Med Chem Lett ; 19(15): 4446-9, 2009 Aug 01.

Article in English | MEDLINE | ID: mdl-19525110

15.

3,4-Diamino-2,5-thiadiazole-1-oxides as potent CXCR2/CXCR1 antagonists.

Biju, Purakkattle; Taveras, Arthur; Yu, Younong; Zheng, Junying; Chao, Jianhua; Rindgen, Diane; Jakway, James; Hipkin, R William; Fossetta, James; Fan, Xuedong; Fine, Jay; Qiu, Hongchen; Merritt, J Robert; Baldwin, John J.

Bioorg Med Chem Lett ; 18(1): 228-31, 2008 Jan 01.

Article in English | MEDLINE | ID: mdl-18006311

16.

Synthesis and structure-activity relationships of heteroaryl substituted-3,4-diamino-3-cyclobut-3-ene-1,2-dione CXCR2/CXCR1 receptor antagonists.

Yu, Younong; Dwyer, Michael P; Chao, Jianping; Aki, Cynthia; Chao, Jianhua; Purakkattle, Biju; Rindgen, Diane; Bond, Richard; Mayer-Ezel, Rosemary; Jakway, James; Qiu, Hongchen; Hipkin, R William; Fossetta, James; Gonsiorek, Waldemar; Bian, Hong; Fan, Xuedong; Terminelli, Carol; Fine, Jay; Lundell, Daniel; Merritt, J Robert; He, Zhenmin; Lai, Gaifa; Wu, Minglang; Taveras, Arthur.

Bioorg Med Chem Lett ; 18(4): 1318-22, 2008 Feb 15.

Article in English | MEDLINE | ID: mdl-18242983

17.

Synthesis of the oxygenated pactamycin core.

Knapp, Spencer; Yu, Younong.

Org Lett ; 9(7): 1359-62, 2007 Mar 29.

Article in English | MEDLINE | ID: mdl-17338541

18.

Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.

Dwyer, Michael P; Yu, Younong; Chao, Jianping; Aki, Cynthia; Chao, Jianhua; Biju, Purakkattle; Girijavallabhan, Viyyoor; Rindgen, Diane; Bond, Richard; Mayer-Ezel, Rosemary; Jakway, James; Hipkin, R William; Fossetta, James; Gonsiorek, Waldemar; Bian, Hong; Fan, Xuedong; Terminelli, Carol; Fine, Jay; Lundell, Daniel; Merritt, J Robert; Rokosz, Laura L; Kaiser, Bernd; Li, Ge; Wang, Wei; Stauffer, Tara; Ozgur, Lynne; Baldwin, John; Taveras, Arthur G.

J Med Chem ; 49(26): 7603-6, 2006 Dec 28.

Article in English | MEDLINE | ID: mdl-17181143

19.

Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.

Liu, Jian; Guiadeen, Deodial; Krikorian, Arto; Gao, Xiaolei; Wang, James; Boga, Sobhana Babu; Alhassan, Abdul-Basit; Yu, Younong; Vaccaro, Henry; Liu, Shilan; Yang, Chundao; Wu, Hao; Cooper, Alan; de Man, Jos; Kaptein, Allard; Maloney, Kevin; Hornak, Viktor; Gao, Ying-Duo; Fischmann, Thierry O; Raaijmakers, Hans; Vu-Pham, Diep; Presland, Jeremy; Mansueto, My; Xu, Zangwei; Leccese, Erica; Zhang-Hoover, Jie; Knemeyer, Ian; Garlisi, Charles G; Bays, Nathan; Stivers, Peter; Brandish, Philip E; Hicks, Alexandra; Kim, Ronald; Kozlowski, Joseph A.

ACS Med Chem Lett ; 7(2): 198-203, 2016 Feb 11.

Article in English | MEDLINE | ID: mdl-26985298

20.

CXCR2 modulators: a patent review (2009 - 2013).

Dwyer, Michael P; Yu, Younong.

Expert Opin Ther Pat ; 24(5): 519-34, 2014 May.

Article in English | MEDLINE | ID: mdl-24555661

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