Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Eric Brian Sjogren"'
Autor:
Mirna Rodriguez, Timothy Friend Stanton, Frances Zhao, Eric Brian Sjogren, Taotao Wang, Jinfu Yang, Matthew I. Gross, Jim Li, Mark K. Bennett, Tania Chernov-Rogan, Julie Janes, Andrew L. Mackinnon, Susan Demo, Guy J. Laidig, Lijing Chen, Bindu Goyal, Francesco Parlati, Jennifer B. Dennison, Peter Shwonek, Evan R. Lewis
Publikováno v:
Molecular Cancer Therapeutics. 13:890-901
Glutamine serves as an important source of energy and building blocks for many tumor cells. The first step in glutamine utilization is its conversion to glutamate by the mitochondrial enzyme glutaminase. CB-839 is a potent, selective, and orally bioa
Autor:
Jaehyeon Park, Harlan F Reese, Yun-Chou Tan, Hasim Zecic, Martin Stahl, Keshab Sarma, Renee Litman, Alejandra Trejo, William Bingenheimer, Michael Soth, David Michael Goldstein, Mary Welch, Eric Brian Sjogren, Man-Ling Sung, Sandra Frauchiger, Nolan James Dewdney, Bong San Pablo, Eva Papp, Daniel McWeeney, Ronald J. Hill, Paul Weller, Manjiri Ghate, JoAnn La Fargue, Brian Wong, Stacie A. Dalrymple, James Patrick Dunn, David Mark Rotstein, Richard T. Roberts, Bradford Graves, Rebecca T Suttman, Mcintosh Joel, Farrell Robert P, Andreas Kuglstatter, Chen Jian Jeffrey, Fujun Li, Humberto Bartolome Arzeno, Brad Loe, Tobias Gabriel
Publikováno v:
Journal of Medicinal Chemistry. 54:2255-2265
The development of a new series of p38α inhibitors resulted in the identification of two clinical candidates, one of which was advanced into a phase 2 clinical study for rheumatoid arthritis. The original lead, an lck inhibitor that also potently in
Autor:
Hanbiao Yang, Eric Brian Sjogren
Publikováno v:
Tetrahedron Letters. 51:3524-3527
The isoquinoline ring system is a reoccurring structural motif in alkaloids 1 and pharmaceuticals. 2 Consequently, the synthesis and functionalization of isoquinolines have attracted considerable attention from the synthetic community. 3 We previousl
Autor:
R.L. Vimont, Lisa M. Gross, Magarita Romero, David E. Clarke, Andrea DeSousa, Wylie Solang Palmer, Nicolas F. Arredondo, Francisco Xavier Talamas, Anthony P.D.W. Ford, D.R. Blue, Gary W. Bantle, Leticia Sandoval, David Bruce Repke, John D Lesnick, Rachel S. Ozer, Alfredo Vazquez, Eric Brian Sjogren, Timothy J. Williams, M. Shannon Kava, David J. Morgans, Quan-Ming Zhu, Helen Y. Wu, Todd R. Elworthy, and Jürg R. Pfister
Publikováno v:
Journal of Medicinal Chemistry. 40:2674-2687
Novel arylpiperazines were identified as alpha 1-adrenoceptor (AR) subtype-selective antagonists by functional in vitro screening. 3-[4-(ortho-Substituted phenyl)piperazin-1-yl]propylamines were derivatized with N,N-dimethyl anthranilamides, nicotina
Autor:
Carlos Gonzalez, Stephen F. Carr, Elsie M. Eugui, Rebecca A. Stephenson, Fidencio Franco, Peter H. Nelson, Ann-Marie Waltos, Eric Brian Sjogren, Sussan Rouhafza, Francisco Xavier Talamas, Ronald Charles Hawley, Devens Bruce H, David G. Loughhead, Robert James Weikert, Patterson John W, Eva Papp, David J. Milan, John C. Wu, David Bernard Smith
Publikováno v:
Journal of Medicinal Chemistry. 39:4181-4196
Structure-activity relationships in the region of the phthalide ring of the inosine monophosphate dehydrogenase inhibitor mycophenolic acid have been explored. Replacement of the lactone ring with other cyclic moieties resulted in loss of potency, es
Autor:
Gill Adrian Liam, Csaba Lehel, Mcintosh Joel, Francisco Xavier Talamas, Roland J. Billedeau, Holger Wesche, David Clark, Eric Brian Sjogren, Matt Wright, Nigel Walker, Stacie A. Dalrymple, Sharada Shenvi Labadie, Camran Parast, Timothy D. Cushing, George Tonn, Michelle F. Browner, Keith A. M. Walker, Viola Bordunov, Pu-Ping Lu, Marie-Louise Smith, Chris Whitehead, Xiao He, Mario G. Cardozo, Juan C. Jaen, Chris Allen Broka, Peng Cheng, Youngsook Shin, Karen Berry, Vijay Baichwal, Shichang Miao, Ronald Charles Hawley, Xiaolin Hao, Michael DeGraffenreid, Marc Labelle
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(1)
A novel series of (E)-1-((2-(1-methyl-1H-imidazol-5-yl) quinolin-4-yl) methylene) thiosemicarbazides was discovered as potent inhibitors of IKKβ. In this Letter we document our early efforts at optimization of the quinoline core, the imidazole and t
Autor:
Karen Berry, Viola Bordunov, Shichang Miao, David Clark, George Tonn, Timothy D. Cushing, Ronald Charles Hawley, Gill Adrian Liam, Marc Labelle, Csaba Lehel, Pu-Ping Lu, Francisco Xavier Talamas, Vijay Baichwal, Roland J. Billedeau, Mario G. Cardozo, Mcintosh Joel, Peng Cheng, Marie-Louise Smith, Michael DeGraffenreid, Chris Whitehead, Stacie A. Dalrymple, Xiao He, Nigel Walker, Camran Parast, Xiaolin Hao, Holger Wesche, Matt Wright, Eric Brian Sjogren, Keith A. M. Walker, Juan C. Jaen, Chris Allen Broka, Sharada Shenvi Labadie, Michelle F. Browner, Youngsook Shin
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(1)
A novel series of (E)-1-((2-(1-methyl-1H-imidazol-5-yl) quinolin-4-yl) methylene) thiosemicarbazides was discovered as potent inhibitors of IKKβ. In this Letter we document our efforts at further optimization of this series, culminating in 2 with su
Autor:
Michael A. Rider, Anthony L. Poulton, Eric Brian Sjogren, Richard Komuniecki, Peter H. Nelson, Stanford Bingham, Mark A. Emanuel
Publikováno v:
Journal of Medicinal Chemistry. 34:3295-3301
A series of alpha-cyano-beta-hydroxypropenamides was prepared and tested for anthelmintic activity. alpha-Cyano-beta-hydroxy-N-[4- (trifluoromethyl)phenyl]-3-[4-(trifluoromethyl)phenyl]propenamide (1) showed good activity against the nematode Nematos
Autor:
Alexander Alanine, Gutknecht Eva-Maria, Wolfgang von der Saal, Shinji Tsujii, Henri Stalder, Michael Patrick Dillon, Mark Rogers-Evans, Jochen Zuegge, Gisbert Schneider, Manfred Kansy, Wolfgang Guba, Petra Schneider, Eric Brian Sjogren, Paul Gillespie, Gerd Zimmermann, Phil Jones, Olivier Roche, Harris William, Werner Neidhart, Mikio Taniguchi, Franck Danel, Nader Fotouhi, Robert Alan Goodnow, Konrad Bleicher
Publikováno v:
Journal of medicinal chemistry. 45(1)
A computer-based method was developed for rapid and automatic identification of potential "frequent hitters". These compounds show up as hits in many different biological assays covering a wide range of targets. A scoring scheme was elaborated from s
Publikováno v:
Journal of Medicinal Chemistry. 28:1673-1679
Screening of mesoionic compounds as potential electron acceptors by analogy with metronidazole led to the finding of in vitro antitrichomonal activity for anhydro-2-phenyl-3-hydroxythiazolo [3,2-a]pyridinium hydroxide (1). In a series of analogues, p