Search Results - "Lin, Shuqun"

Design, Synthesis, and Anti-inflammatory Properties of Orally Active 4-(Phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38α Mitogen-Activated Protein Kinase Inhibitors by Hynes, John, Dyckman, Alaric J, Lin, Shuqun, Wrobleski, Stephen T, Wu, Hong, Gillooly, Kathleen M, Kanner, Steven B, Lonial, Herinder, Loo, Derek, McIntyre, Kim W, Pitt, Sidney, Shen, Ding Ren, Shuster, David J, Yang, XiaoXia, Zhang, Rosemary, Behnia, Kamelia, Zhang, Hongjian, Marathe, Punit H, Doweyko, Arthur M, Tokarski, John S, Sack, John S, Pokross, Matthew, Kiefer, Susan E, Newitt, John A, Barrish, Joel C, Dodd, John, Schieven, Gary L, Leftheris, Katerina

“…A novel structural class of p38 mitogen-activated protein (MAP) kinase inhibitors consisting of substituted 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazines has…”
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Utilization of a nitrogen–sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors by Lin, Shuqun, Wrobleski, Stephen T., Hynes, John, Pitt, Sidney, Zhang, Rosemary, Fan, Yi, Doweyko, Arthur M., Kish, Kevin F., Sack, John S., Malley, Mary F., Kiefer, Susan E., Newitt, John A., McKinnon, Murray, Trzaskos, James, Barrish, Joel C., Dodd, John H., Schieven, Gary L., Leftheris, Katerina

“…An intramolecular nitrogen–sulfur nonbonding interaction has been used in the design of a novel series of 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase…”
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Synthesis and SAR of new pyrrolo[2,1- f][1,2,4]triazines as potent p38α MAP kinase inhibitors by Wrobleski, Stephen T., Lin, Shuqun, Hynes, John, Wu, Hong, Pitt, Sidney, Shen, Ding Ren, Zhang, Rosemary, Gillooly, Kathleen M., Shuster, David J., McIntyre, Kim W., Doweyko, Arthur M., Kish, Kevin F., Tredup, Jeffrey A., Duke, Gerald J., Sack, John S., McKinnon, Murray, Dodd, John, Barrish, Joel C., Schieven, Gary L., Leftheris, Katerina

“…Synthesis of a novel series of substituted pyrrolo[2,1- f][1,2,4]triazines have resulted in the identification of subnanomolar inhibitors of the p38α MAP…”
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Synthesis and SAR of p38α MAP kinase inhibitors based on heterobicyclic scaffolds by Murali Dhar, T.G., Wrobleski, Stephen T., Lin, Shuqun, Furch, Joseph A., Nirschl, David S., Fan, Yi, Todderud, Gordon, Pitt, Sidney, Doweyko, Arthur M., Sack, John S., Mathur, Arvind, McKinnon, Murray, Barrish, Joel C., Dodd, John H., Schieven, Gary L., Leftheris, Katerina

“…The synthesis and structure–activity relationships (SAR) of p38α MAP kinase inhibitors based on heterobicyclic scaffolds are described. This effort led to the…”
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The Discovery of Orally Active Triaminotriazine Aniline Amides as Inhibitors of p38 MAP Kinase by Leftheris, Katerina, Ahmed, Gulzar, Chan, Ran, Dyckman, Alaric J, Hussain, Zahid, Ho, Kan, Hynes, John, Letourneau, Jeffrey, Li, Wei, Lin, Shuqun, Metzger, Axel, Moriarty, Kevin J, Riviello, Chris, Shimshock, Yvonne, Wen, James, Wityak, John, Wrobleski, Stephen T, Wu, Hong, Wu, Junjun, Desai, Madhuri, Gillooly, Kathleen M, Lin, Tsung H, Loo, Derek, McIntyre, Kim W, Pitt, Sidney, Shen, Ding Ren, Shuster, David J, Zhang, Rosemary, Diller, David, Doweyko, Arthur, Sack, John, Baldwin, Jack, Barrish, Joel, Dodd, John, Henderson, Ian, Kanner, Steve, Schieven, Gary L, Webb, Maria

“…A new structural class of triaminotriazine aniline amides possessing potent p38 enzyme activity has been discovered. The initial hit (compound 1a) was…”
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Rational Design and Synthesis of an Orally Active Indolopyridone as a Novel Conformationally Constrained Cannabinoid Ligand Possessing Antiinflammatory Properties by Wrobleski, Stephen T, Chen, Ping, Hynes, John, Lin, Shuqun, Norris, Derek J, Pandit, Chennagiri R, Spergel, Steven, Wu, Hong, Tokarski, John S, Chen, Xiaorong, Gillooly, Kathleen M, Kiener, Peter A, McIntyre, Kim W, Patil-koota, Vina, Shuster, David J, Turk, Lori A, Yang, Guchen, Leftheris, Katerina

“…A series of unique indazoles and pyridoindolones have been rationally designed and synthesized as novel classes of cannabinoid ligands based on a proposed…”
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Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains by Zhao, Chen, Sham, Hing L., Sun, Minghua, Stoll, Vincent S., Stewart, Kent D., Lin, Shuqun, Mo, Hongmei, Vasavanonda, Sudthida, Saldivar, Ayda, Park, Chang, McDonald, Edith J., Marsh, Kennan C., Klein, Larry L., Kempf, Dale J., Norbeck, Daniel W.

“…As part of our efforts to identify potent HIV-1 protease inhibitors that are active against resistant viral strains, structural modification of the azacyclic…”
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Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165 by Wrobleski, Stephen T, Moslin, Ryan, Lin, Shuqun, Zhang, Yanlei, Spergel, Steven, Kempson, James, Tokarski, John S, Strnad, Joann, Zupa-Fernandez, Adriana, Cheng, Lihong, Shuster, David, Gillooly, Kathleen, Yang, Xiaoxia, Heimrich, Elizabeth, McIntyre, Kim W, Chaudhry, Charu, Khan, Javed, Ruzanov, Max, Tredup, Jeffrey, Mulligan, Dawn, Xie, Dianlin, Sun, Huadong, Huang, Christine, D’Arienzo, Celia, Aranibar, Nelly, Chiney, Manoj, Chimalakonda, Anjaneya, Pitts, William J, Lombardo, Louis, Carter, Percy H, Burke, James R, Weinstein, David S

“…Small molecule JAK inhibitors have emerged as a major therapeutic advancement in treating autoimmune diseases. The discovery of isoform selective JAK…”
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Identification of N‑Methyl Nicotinamide and N‑Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2) by Moslin, Ryan, Zhang, Yanlei, Wrobleski, Stephen T, Lin, Shuqun, Mertzman, Michael, Spergel, Steven, Tokarski, John S, Strnad, Joann, Gillooly, Kathleen, McIntyre, Kim W, Zupa-Fernandez, Adriana, Cheng, Lihong, Sun, Huadong, Chaudhry, Charu, Huang, Christine, D’Arienzo, Celia, Heimrich, Elizabeth, Yang, Xiaoxia, Muckelbauer, Jodi K, Chang, ChiehYing, Tredup, Jeffrey, Mulligan, Dawn, Xie, Dianlin, Aranibar, Nelly, Chiney, Manoj, Burke, James R, Lombardo, Louis, Carter, Percy H, Weinstein, David S

“…As a member of the Janus (JAK) family of nonreceptor tyrosine kinases, TYK2 plays an important role in mediating the signaling of pro-inflammatory cytokines…”
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A Novel, Picomolar Inhibitor of Human Immunodeficiency Virus Type 1 Protease by Sham, Hing L, Zhao, Chen, Stewart, Kent D, Betebenner, David A, Lin, Shuqun, Park, Chang H, Kong, Xiang-P, Rosenbrook, William, Herrin, Thomas, Madigan, Darold, Vasavanonda, Suthida, Lyons, Nicholas, Molla, Akhter, Saldivar, Ayda, Marsh, Kennan C, McDonald, Edith, Wideburg, Norman E, Denissen, Jon F, Robins, Terrel, Kempf, Dale J, Plattner, Jacob J, Norbeck, Daniel W

“…The design, synthesis, and molecular modeling studies of a novel series of azacyclic ureas, which are inhibitors of human immunodeficiency virus type 1 (HIV-1)…”
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Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors by Bhide, Rajeev S., Keon, Alec, Weigelt, Carolyn, Sack, John S., Schmidt, Robert J., Lin, Shuqun, Xiao, Hai-Yun, Spergel, Steven H., Kempson, James, Pitts, William J., Carman, Julie, Poss, Michael A.

“…[Display omitted] The identification of small molecule inhibitors of IRAK4 for the treatment of autoimmune diseases has been an area of intense research. We…”
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Discovery of highly potent, selective, covalent inhibitors of JAK3 by Kempson, James, Ovalle, Damaso, Guo, Junqing, Wrobleski, Stephen T., Lin, Shuqun, Spergel, Steven H., Duan, James J.-W., Jiang, Bin, Lu, Zhonghui, Das, Jagabandhu, Yang, Bingwei V., Hynes, John, Wu, Hong, Tokarski, John, Sack, John S., Khan, Javed, Schieven, Gary, Blatt, Yuval, Chaudhry, Charu, Salter-Cid, Luisa M., Fura, Aberra, Barrish, Joel C., Carter, Percy H., Pitts, William J.

“…[Display omitted] A useful and novel set of tool molecules have been identified which bind irreversibly to the JAK3 active site cysteine residue. The design…”
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Novel advances in biotransformation and bioactivation research - 2020 year in review by Khojasteh, S. Cyrus, Argikar, Upendra A., Driscoll, James P., Heck, Carley J. S., King, Lloyd, Jackson, Klarissa D., Jian, Wenying, Kalgutkar, Amit S., Miller, Grover P., Kramlinger, Valerie, Rietjens, Ivonne M. C. M., Teitelbaum, Aaron M., Wang, Kai, Wei, Cong

“…This annual review is the sixth of its kind since 2016 (see references). Our objective is to explore and share articles which we deem influential and…”
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Discovery of 4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a Clinical p38α MAP Kinase Inhibitor for the Treatment of Inflammatory Diseases by Liu, Chunjian, Lin, James, Wrobleski, Stephen T, Lin, Shuqun, Hynes, John, Wu, Hong, Dyckman, Alaric J, Li, Tianle, Wityak, John, Gillooly, Kathleen M, Pitt, Sidney, Shen, Ding Ren, Zhang, Rosemary F, McIntyre, Kim W, Salter-Cid, Luisa, Shuster, David J, Zhang, Hongjian, Marathe, Punit H, Doweyko, Arthur M, Sack, John S, Kiefer, Susan E, Kish, Kevin F, Newitt, John A, McKinnon, Murray, Dodd, John H, Barrish, Joel C, Schieven, Gary L, Leftheris, Katerina

“…The discovery and characterization of 7k (BMS-582949), a highly selective p38α MAP kinase inhibitor that is currently in phase II clinical trials for the…”
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Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors by Duan, James J-W, Lu, Zhonghui, Jiang, Bin, Yang, Bingwei V, Doweyko, Lidia M, Nirschl, David S, Haque, Lauren E, Lin, Shuqun, Brown, Gregory, Hynes, Jr, John, Tokarski, John S, Sack, John S, Khan, Javed, Lippy, Jonathan S, Zhang, Rosemary F, Pitt, Sidney, Shen, Guoxiang, Pitts, William J, Carter, Percy H, Barrish, Joel C, Nadler, Steven G, Salter-Cid, Luisa M, McKinnon, Murray, Fura, Aberra, Schieven, Gary L, Wrobleski, Stephen T

“…A new class of Janus kinase (JAK) inhibitors was discovered using a rationally designed pyrrolo[1,2-b]pyridazine-3-carboxamide scaffold. Preliminary studies…”
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Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor by Liu, Chunjian, Lin, James, Hynes, John, Wu, Hong, Wrobleski, Stephen T, Lin, Shuqun, Dhar, T G Murali, Vrudhula, Vivekananda M, Sun, Jung-Hui, Chao, Sam, Zhao, Rulin, Wang, Bei, Chen, Bang-Chi, Everlof, Gerry, Gesenberg, Christoph, Zhang, Hongjian, Marathe, Punit H, McIntyre, Kim W, Taylor, Tracy L, Gillooly, Kathleen, Shuster, David J, McKinnon, Murray, Dodd, John H, Barrish, Joel C, Schieven, Gary L, Leftheris, Katerina

“…In search for prodrugs to address the issue of pH-dependent solubility and exposure associated with 1 (BMS-582949), a previously disclosed phase II clinical…”
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Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2‑f][1,2,4]triazine-6-carbonyl)­(propyl)­carba­moyl­oxy)­methyl-2-(4-(phos­pho­no­oxy)­phenyl)­acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor by Liu, Chunjian, Lin, James, Hynes, John, Wu, Hong, Wrobleski, Stephen T., Lin, Shuqun, Dhar, T. G. Murali, Vrudhula, Vivekananda M., Sun, Jung-Hui, Chao, Sam, Zhao, Rulin, Wang, Bei, Chen, Bang-Chi, Everlof, Gerry, Gesenberg, Christoph, Zhang, Hongjian, Marathe, Punit H., McIntyre, Kim W., Taylor, Tracy L., Gillooly, Kathleen, Shuster, David J., McKinnon, Murray, Dodd, John H., Barrish, Joel C., Schieven, Gary L., Leftheris, Katerina

“…In search for prodrugs to address the issue of pH-dependent solubility and exposure associated with 1 (BMS-582949), a previously disclosed phase II clinical…”
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Novel Azacyclic Ureas That Are Potent Inhibitors of HIV-1 Protease by Sham, Hing L., Zhao, Chen, Marsh, Kennan C., Betebenner, David A., Lin, Shuqun, Jr, William Rosenbrook, Herrin, Thomas, Li, Leping, Madigan, Darold, Vasavanonda, Suthida, Molla, Akhter, Saldivar, Ayda, McDonald, Edith, Wideburg, Norman E., Kempf, Dale, Norbeck, Daniel W., Plattner, Jacob J.

“…A series of novel, azacyclic ureas which are highly potent inhibitors of the HIV-1 protease (IC50= 4.1 to <0.5 nM) were synthesized. Aqueous solubilities of…”
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The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode by Wrobleski, Stephen T., Lin, Shuqun, Murali Dhar, T.G., Dyckman, Alaric J., Li, Tianle, Pitt, Sidney, Zhang, Rosemary, Fan, Yi, Doweyko, Arthur M., Tokarski, John S., Kish, Kevin F., Kiefer, Susan E., Sack, John S., Newitt, John A., Witmer, Mark R., McKinnon, Murray, Barrish, Joel C., Dodd, John H., Schieven, Gary L., Leftheris, Katerina

“…A novel series of p38 MAP kinase inhibitors with high selectivity for the p38α isoform over the other family members including the highly homologous p38β…”
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The identification of novel p38I- isoform selective kinase inhibitors having an unprecedented p38I- binding mode by Wrobleski, Stephen, Lin, Shuqun, Dhar, T G, Dyckman, Alaric, Li, Tianle, Pitt, Sidney, Zhang, Rosemary, Fan, Yi, Doweyko, Arthur, Tokarski, John, Kish, Kevin, Kiefer, Susan, Sack, John, Newitt, John, Witmer, Mark, McKinnon, Murray, Barrish, Joel, Dodd, John, Schieven, Gary, Leftheris, Katerina

“…A novel series of p38 MAP kinase inhibitors with high selectivity for the p38I- isoform over the other family members including the highly homologous p38I2…”
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