Discovery and optimization of new oxadiazole substituted thiazole RORγt inverse agonists through a bioisosteric amide replacement approach
Steeneck, Christoph, Gege, Christian, Kinzel, Olaf, Albers, Michael, Kleymann, Gerald, Schlüter, Thomas, Schulz, Andreas, Xue, Xiaohua, Cummings, Maxwell D., Fourie, Anne M., Leonard, Kristi A., Scott, Brian, Edwards, James P., Hoffmann, Thomas, Goldberg, Steven D.
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Published in Bioorganic & medicinal chemistry letters (15.06.2020)
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Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease
Leonard, Kristi A, Madge, Lisa A, Krawczuk, Paul J, Wang, Aihua, Kreutter, Kevin D, Bacani, Genesis M, Chai, Wenying, Smith, Russell C, Tichenor, Mark S, Harris, Michael C, Malaviya, Ravi, Seierstad, Mark, Johnson, Marguerite E, Venable, Jennifer D, Kim, Suzie, Hirst, Gavin C, Mathur, Ashok S, Rao, Tadimeti S, Edwards, James P, Rizzolio, Michele C, Koudriakova, Tatiana
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Published in Journal of medicinal chemistry (26.03.2020)
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Discovery of a Potent and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase with Oral Anti-Inflammatory Activity
Tichenor, Mark S, Wiener, John J. M, Rao, Navin L, Pooley Deckhut, Charlotte, Barbay, J. Kent, Kreutter, Kevin D, Bacani, Genesis M, Wei, Jianmei, Chang, Leon, Murrey, Heather E, Wang, Weixue, Ahn, Kay, Huber, Michael, Rex, Elizabeth, Coe, Kevin J, Wu, JieJun, Seierstad, Mark, Bembenek, Scott D, Leonard, Kristi A, Lebsack, Alec D, Venable, Jennifer D, Edwards, James P
Published in ACS medicinal chemistry letters (13.05.2021)
Published in ACS medicinal chemistry letters (13.05.2021)
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Design, Synthesis, and Biological Evaluation of Novel Potent and Selective αvβ3/αvβ5 Integrin Dual Inhibitors with Improved Bioavailability. Selection of the Molecular Core
Marugán, Juan José, Manthey, Carl, Anaclerio, Beth, Lafrance, Lou, Lu, Tianbao, Markotan, Tom, Leonard, Kristi A, Crysler, Carl, Eisennagel, Stephen, Dasgupta, Malini, Tomczuk, Bruce
Published in Journal of medicinal chemistry (24.02.2005)
Published in Journal of medicinal chemistry (24.02.2005)
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A Transient N−O-Linked Pauson−Khand Strategy for the Synthesis of the Deschloro Carbocyclic Core of the Palau'amines and Styloguanidines
Koenig, Stefan G, Miller, Stefan M, Leonard, Kristi A, Löwe, Ralf S, Chen, Betty C, Austin, David J
Published in Organic letters (26.06.2003)
Published in Organic letters (26.06.2003)
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2,4,6-Triarylchalcogenopyrylium Dyes Related in Structure to the Antitumor Agent AA1 as in Vitro Sensitizers for the Photodynamic Therapy of Cancer
Leonard, Kristi A, Nelen, Marina I, Anderson, Linda T, Gibson, Scott L, Hilf, Russell, Detty, Michael R
Published in Journal of medicinal chemistry (23.09.1999)
Published in Journal of medicinal chemistry (23.09.1999)
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A Selenopyrylium Photosensitizer for Photodynamic Therapy Related in Structure to the Antitumor Agent AA1 with Potent in Vivo Activity and No Long-Term Skin Photosensitization
Leonard, Kristi A, Hall, Jonathan P, Nelen, Marina I, Davies, Sherry R, Gollnick, Sandra O, Camacho, Sue, Oseroff, Allan R, Gibson, Scott L, Hilf, Russell, Detty, Michael R
Published in Journal of medicinal chemistry (16.11.2000)
Published in Journal of medicinal chemistry (16.11.2000)
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Synthesis and Evaluation of Chalcogenopyrylium Dyes as Potential Sensitizers for the Photodynamic Therapy of Cancer
Leonard, Kristi A, Nelen, Marina I, Simard, Todd P, Davies, Sherry R, Gollnick, Sandra O, Oseroff, Allan R, Gibson, Scott L, Hilf, Russell, Chen, Lan Bo, Detty, Michael R
Published in Journal of medicinal chemistry (23.09.1999)
Published in Journal of medicinal chemistry (23.09.1999)
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Discovery of a highly selective chemical inhibitor of matrix metalloproteinase-9 (MMP-9) that allosterically inhibits zymogen activation
Scannevin, Robert H., Alexander, Richard, Haarlander, Tara Mezzasalma, Burke, Sharon L., Singer, Monica, Huo, Cuifen, Zhang, Yue-Mei, Maguire, Diane, Spurlino, John, Deckman, Ingrid, Carroll, Karen I., Lewandowski, Frank, Devine, Eric, Dzordzorme, Keli, Tounge, Brett, Milligan, Cindy, Bayoumy, Shariff, Williams, Robyn, Schalk-Hihi, Celine, Leonard, Kristi, Jackson, Paul, Todd, Matthew, Kuo, Lawrence C., Rhodes, Kenneth J.
Published in The Journal of biological chemistry (27.10.2017)
Published in The Journal of biological chemistry (27.10.2017)
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Pharmacologic modulation of RORγt translates to efficacy in preclinical and translational models of psoriasis and inflammatory arthritis
Xue, Xiaohua, Soroosh, Pejman, De Leon-Tabaldo, Aimee, Luna-Roman, Rosa, Sablad, Marciano, Rozenkrants, Natasha, Yu, Jingxue, Castro, Glenda, Banie, Homayon, Fung-Leung, Wai-Ping, Santamaria-Babi, Luis, Schlueter, Thomas, Albers, Michael, Leonard, Kristi, Budelsky, Alison L., Fourie, Anne M.
Published in Scientific reports (01.12.2016)
Published in Scientific reports (01.12.2016)
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Optimization and biological evaluation of thiazole-bis-amide inverse agonists of RORγt
Gege, Christian, Albers, Michael, Kinzel, Olaf, Kleymann, Gerald, Schlüter, Thomas, Steeneck, Christoph, Hoffmann, Thomas, Xue, Xiaohua, Cummings, Maxwell D., Spurlino, John, Milligan, Cynthia, Fourie, Anne M., Edwards, James P., Leonard, Kristi, Coe, Kevin, Scott, Brian, Pippel, Dan, Goldberg, Steven D.
Published in Bioorganic & medicinal chemistry letters (15.06.2020)
Published in Bioorganic & medicinal chemistry letters (15.06.2020)
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Journal Article
Identification and biological evaluation of thiazole-based inverse agonists of RORγt
Gege, Christian, Cummings, Maxwell D., Albers, Michael, Kinzel, Olaf, Kleymann, Gerald, Schlüter, Thomas, Steeneck, Christoph, Nelen, Marina I., Milligan, Cindy, Spurlino, John, Xue, Xiaohua, Leonard, Kristi, Edwards, James P., Fourie, Anne, Goldberg, Steven D., Hoffmann, Thomas
Published in Bioorganic & medicinal chemistry letters (15.05.2018)
Published in Bioorganic & medicinal chemistry letters (15.05.2018)
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Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt
Kummer, David A., Cummings, Maxwell D., Abad, Marta, Barbay, Joseph, Castro, Glenda, Wolin, Ronald, Kreutter, Kevin D., Maharoof, Umar, Milligan, Cynthia, Nishimura, Rachel, Pierce, Joan, Schalk-Hihi, Celine, Spurlino, John, Urbanski, Maud, Venkatesan, Hariharan, Wang, Aihua, Woods, Craig, Xue, Xiaohua, Edwards, James P., Fourie, Anne M., Leonard, Kristi
Published in Bioorganic & medicinal chemistry letters (01.05.2017)
Published in Bioorganic & medicinal chemistry letters (01.05.2017)
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6-Substituted quinolines as RORγt inverse agonists
Barbay, J. Kent, Cummings, Maxwell D., Abad, Marta, Castro, Glenda, Kreutter, Kevin D., Kummer, David A., Maharoof, Umar, Milligan, Cynthia, Nishimura, Rachel, Pierce, Joan, Schalk-Hihi, Celine, Spurlino, John, Tanis, Virginia M., Urbanski, Maud, Venkatesan, Hariharan, Wang, Aihua, Woods, Craig, Wolin, Ronald, Xue, Xiaohua, Edwards, James P., Fourie, Anne M., Leonard, Kristi
Published in Bioorganic & medicinal chemistry letters (01.12.2017)
Published in Bioorganic & medicinal chemistry letters (01.12.2017)
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3-Substituted Quinolines as RORγt Inverse Agonists
Tanis, Virginia M., Venkatesan, Hariharan, Cummings, Maxwell D., Albers, Michael, Kent Barbay, J., Herman, Krystal, Kummer, David A., Milligan, Cynthia, Nelen, Marina I., Nishimura, Rachel, Schlueter, Thomas, Scott, Brian, Spurlino, John, Wolin, Ronald, Woods, Craig, Xue, Xiaohua, Edwards, James P., Fourie, Anne M., Leonard, Kristi
Published in Bioorganic & medicinal chemistry letters (15.06.2019)
Published in Bioorganic & medicinal chemistry letters (15.06.2019)
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Design and Characterization of Optimized Adenosine A(2A)/A(1) Receptor Antagonists for the Treatment of Parkinson's Disease
Shook, Brian C., Rassnick, Stefanie, Wallace, Nathaniel, Crooke, Jeffrey, Ault, Mark, Chakravarty, Devraj, Barbay, J. Kent, Wang, Aihua, Powell, Mark T., Leonard, Kristi, Alford, Vernon, Scannevin, Robert H., Carroll, Karen, Lampron, Lisa, Westover, Lori, Lim, Heng-Keang, Russell, Ronald, Branum, Shawn, Wells, Kenneth M., Damon, Sandra, Youells, Scott, Li, Xun, Beauchamp, Derek A., Rhodes, Kenneth, Jackson, Paul F.
Published in Journal of medicinal chemistry (09.02.2012)
Published in Journal of medicinal chemistry (09.02.2012)
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Substituted thieno[2,3-d]pyrimidines as adenosine A(2A) receptor antagonists
Shook, Brian C., Chakravarty, Devraj, Barbay, J. Kent, Wang, Aihua, Leonard, Kristi, Alford, Vernon, Powell, Mark T., Rassnick, Stefanie, Scannevin, Robert H., Carroll, Karen, Wallace, Nathaniel, Crooke, Jeffrey, Ault, Mark, Lampron, Lisa, Westover, Lori, Rhodes, Kenneth, Jackson, Paul F.
Published in Bioorganic & medicinal chemistry letters (01.05.2013)
Published in Bioorganic & medicinal chemistry letters (01.05.2013)
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Journal Article
Design and Characterization of Optimized Adenosine A 2A /A 1 Receptor Antagonists for the Treatment of Parkinson's Disease
Shook, Brian C., Rassnick, Stefanie, Wallace, Nathaniel, Crooke, Jeffrey, Ault, Mark, Chakravarty, Devraj, Barbay, J. Kent, Wang, Aihua, Powell, Mark T., Leonard, Kristi, Alford, Vernon, Scannevin, Robert H., Carroll, Karen, Lampron, Lisa, Westover, Lori, Lim, Heng-Keang, Russell, Ronald, Branum, Shawn, Wells, Kenneth M., Damon, Sandra, Youells, Scott, Li, Xun, Beauchamp, Derek A., Rhodes, Kenneth, Jackson, Paul F.
Published in Journal of medicinal chemistry (09.02.2012)
Published in Journal of medicinal chemistry (09.02.2012)
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