Search Results - "Lynch, Stephen M."

Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors by Jaime-Figueroa, Saul, De Vicente, Javier, Hermann, Johannes, Jahangir, Alam, Jin, Sue, Kuglstatter, Andreas, Lynch, Stephen M., Menke, John, Niu, Linghao, Patel, Vaishali, Shao, Ada, Soth, Michael, Vu, Minh Diem, Yee, Calvin

“…We report the discovery of a novel series of ATP-competitive Janus kinase 3 (JAK3) inhibitors based on the 5H-pyrrolo[2,3-b]pyrazine scaffold. The initial…”
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Molecular pharmacology and antitumor activity of palmarumycin-based inhibitors of thioredoxin reductase by Powis, Garth, Wipf, Peter, Lynch, Stephen M, Birmingham, Anne, Kirkpatrick, D Lynn

“…The cytosolic thioredoxin redox system composed of thioredoxin-1 and the NADPH-dependent thioredoxin reductase-1 reductase is an important regulator of cell…”
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Natural product based inhibitors of the thioredoxin-thioredoxin reductase system by Wipf, Peter, Lynch, Stephen M, Birmingham, Anne, Tamayo, Giselle, Jiménez, Allan, Campos, Nefertiti, Powis, Garth

“…Spiroketal naphthodecalins are readily assembled by Barton's base mediated Ullmann binaphthyl ether coupling, Dakin reactions and hypervalent iodine…”
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Synthesis of Highly Oxygenated Dinaphthyl Ethers via SNAr Reactions Promoted by Barton's Base by Wipf, Peter, Lynch, Stephen M

“…Electron-rich dinaphthyl ethers were synthesized by SNAr reactions between naphthols and activated fluoronaphthalenes…”
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Dibenzazepines and dibenzoxazepines as sodium channel blockers by Lynch, Stephen M., Tafesse, Laykea, Carlin, Kevin, Ghatak, Parijat, Kyle, Donald J.

“…[Display omitted] We have identified two related series of dibenzazepine and dibenzoxazepine sodium channel blockers, which showed good potency on Nav1.7 in…”
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N-Aryl azacycles as novel sodium channel blockers by Lynch, Stephen M., Tafesse, Laykea, Carlin, Kevin, Ghatak, Parijat, Shao, Bin, Abdelhamid, Haissam, Kyle, Donald J.

“…[Display omitted] We have identified a new series of N-aryl azacycles as sodium channel blockers, which showed good potency on Nav1.7 in FLIPR-based and…”
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Pyrrolopyrazines as Selective Spleen Tyrosine Kinase Inhibitors by Padilla, Fernando, Bhagirath, Niala, Chen, Shaoqing, Chiao, Eric, Goldstein, David M, Hermann, Johannes C, Hsu, Jonathan, Kennedy-Smith, Joshua J, Kuglstatter, Andreas, Liao, Cheng, Liu, Wenjian, Lowrie, Lee E, Luk, Kin Chun, Lynch, Stephen M, Menke, John, Niu, Linghao, Owens, Timothy D, O-Yang, Counde, Railkar, Aruna, Schoenfeld, Ryan C, Slade, Michelle, Steiner, Sandra, Tan, Yun-Chou, Villaseñor, Armando G, Wang, Ce, Wanner, Jutta, Xie, Wenwei, Xu, Daigen, Zhang, Xiaohu, Zhou, Mingyan, Lucas, Matthew C

“…We describe the discovery of several pyrrolopyrazines as potent and selective Syk inhibitors and the efforts that eventually led to the desired improvements in…”
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Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome by Lynch, Stephen M., DeVicente, Javier, Hermann, Johannes C., Jaime-Figueroa, Saul, Jin, Sue, Kuglstatter, Andreas, Li, Hongju, Lovey, Allen, Menke, John, Niu, Linghao, Patel, Vaishali, Roy, Douglas, Soth, Michael, Steiner, Sandra, Tivitmahaisoon, Parcharee, Vu, Minh Diem, Yee, Calvin

“…Using a structure based design approach we have identified a series of indazole substituted pyrrolopyrazines, which are potent inhibitors of JAK3…”
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Cycloaddition Chemistry of 2-Vinyl-Substituted Indoles and Related Heteroaromatic Systems by Padwa, Albert, Lynch, Stephen M., Mejía-Oneto, José M., Zhang, Hongjun

“…The intramolecular Diels−Alder cycloaddition reaction (IMDAF) of several N-phenylsulfonylindolyl-substituted furanyl carbamates containing a tethered π-bond on…”
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Design, synthesis, and biological evaluation of new monoamine reuptake inhibitors with potential therapeutic utility in depression and pain by Lucas, Matthew C., Weikert, Robert J., Carter, David S., Cai, Hai-Ying, Greenhouse, Robert, Iyer, Pravin S., Lin, Clara J., Lee, Eun Kyung, Madera, Ann Marie, Moore, Amy, Ozboya, Kerem, Schoenfeld, Ryan C., Steiner, Sandra, Zhai, Yansheng, Lynch, Stephen M.

“…Two new series of monoamine triple reuptake inhibitors (TRIs) have been discovered through scaffold homologation of our recently reported series of…”
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A New Construct of the cis-3a-Aryloctahydroindole Skeleton via the [4+2] Cycloaddition of Furanyl Carbamates by Padwa, Albert, K. Eidell, Cheryl, M. Lynch, Stephen

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Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors by BANNWART, Linda M, CARTER, David S, LYNCH, Stephen M, MADERA, Ann Marie, MOORE, Amy, OZBOYA, Kerem, RAPTOVA, Lubica, ROETZ, Ralf, SCHOENFELD, Ryan C, STEIN, Karin Ann, STEINER, Sandra, VILLA, Marzia, CAI, Hai-Ying, WEIKERT, Robert J, YANSHENG ZHAI, CHOY, Jason C, GREENHOUSE, Robert, JAIME-FIGUEROA, Saul, LYER, Pravin S, LIN, Clara J, EUN KYUNG LEE, LUCAS, Matthew C

“…A series of 3,3-disubstituted pyrrolidine monoamine triple reuptake inhibitors were discovered. Analogues with low nanomolar potency, good human in vitro…”
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Intramolecular Amidofuran Cycloadditions across an Indole π-Bond:  An Efficient Approach to the Aspidosperma and Strychnos ABCE Core by Lynch, Stephen M, Bur, Scott K, Padwa, Albert

“…The intramolecular Diels−Alder reaction between an amidofuran moiety tethered onto an indole component was examined as a strategy for the synthesis of…”
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A New Strategy toward Indole Alkaloids Involving an Intramolecular Cycloaddition/Rearrangement Cascade by Padwa, Albert, Brodney, Michael A, Lynch, Stephen M, Rashatasakhon, Paitoon, Wang, Qiu, Zhang, Hongjun

“…The intramolecular Diels−Alder reaction between an amidofuran moiety tethered onto an indole component was examined as a strategy for the synthesis of…”
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Influence of Ground-State Conformations on the Intramolecular Amidofuran Diels−Alder Reaction by Bur, Scott K, Lynch, Stephen M, Padwa, Albert

“…Various factors that influence the rate of the intramolecular Diels−Alder reaction of amidofurans were investigated with density functional theory calculations…”
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Synthesis and biological activity of prodrug inhibitors of the thioredoxin-thioredoxin reductase system by Wipf, Peter, Lynch, Stephen M, Powis, Garth, Birmingham, Anne, Englund, Erikah E

“…A series of palmarumycin prodrugs and water-soluble analogs has been synthesized and assayed for inhibition of the thioredoxin-thioredoxin reductase system…”
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Synthesis of Azapolycyclic Systems via the Intramolecular [4 + 2] Cycloaddition Chemistry of 2-(Alkylthio)-5-amidofurans by Padwa, Albert, Ginn, John D, Bur, Scott K, Eidell, Cheryl K, Lynch, Stephen M

“…A series of 2-(methylthio)-5-amidofurans containing tethered unsaturation were prepared via the reaction of dimethyl(methylthio)sulfonium tetrafluoroborate…”
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Application of the tandem thionium/N-acyliminium ion cascade toward heterocyclic synthesis by Padwa, Albert, Danca, Diana M., Ginn, John D., Lynch, Stephen M.

“…Many structurally diverse heterocyclic compounds can be easily accessed via the domino Pummerer/cycloaddition/N-acyliminium ion cyclization cascade…”
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Synthesis of Highly Oxygenated Dinaphthyl Ethers via S N Ar Reactions Promoted by Barton's Base by Wipf, Peter, Lynch, Stephen M.

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Formal Total Synthesis of (±)-γ-Lycorane and (±)-1-Deoxylycorine Using the [4+2]-Cycloaddition/Rearrangement Cascade of Furanyl Carbamates by Padwa, Albert, Brodney, Michael A., Lynch, Stephen M.

“…The total syntheses of γ-lycorane and (±)-1-deoxylycorine were accomplished using an intramolecular Diels−Alder cycloaddition of a furanyl carbamate as the key…”
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