Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Stephan C. Schürer"'
Autor:
Daniel J. Cooper, Stephan C. Schürer
Publikováno v:
Molecules
Volume 24
Issue 8
Molecules, Vol 24, Iss 8, p 1604 (2019)
Volume 24
Issue 8
Molecules, Vol 24, Iss 8, p 1604 (2019)
The Toxicology in the 21st Century (Tox21) project seeks to develop and test methods for high-throughput examination of the effect certain chemical compounds have on biological systems. Although primary and toxicity assay data were readily available
Autor:
Ronald J. Rahaim, Yoshihiko Noguchi, Yangbo Feng, Shima Nakanishi, Lin Li, Konstantin Licht, Laura H. Rosenberg, Weimin Chen, John L. Cleveland, Stephan C. Schürer, William R. Roush, Jun Yong Choi, Michael D. Cameron, Mathieu Bibian, Derek R. Duckett
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:4374-4380
The development of a series of potent and highly selective casein kinase 1δ/e (CK1δ/e) inhibitors is described. Starting from a purine scaffold inhibitor (SR-653234) identified by high throughput screening, we developed a series of potent and highl
Autor:
Philip LoGrasso, Thomas D. Bannister, Claudia Ruiz, Thomas Schröter, E. Hampton Sessions, Sarwat Chowdhury, Michael D. Cameron, Stephan C. Schürer, Wayne Grant, Jennifer Pocas, Li Lin, Yangbo Feng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:7107-7112
Rho kinase (ROCK) inhibitors are potential therapeutic agents to treat disorders such as hypertension, multiple sclerosis, cancers, and glaucoma. Here, we disclose the synthesis, optimization, biological evaluation of potent indole and 7-azaindole ba
Autor:
Mohd Hafeez Faridi, Ruth Day, Vineet Gupta, Darren Stoub, Constantinos J. Barth, Stephan C. Schürer, Dony Maiguel
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6902-6906
We report the identification of novel small molecule agonists of integrin CD11b/CD18, which increased, in a dose-dependent manner, the adhesion of the integrin CD11b/CD18 expressing cells to two physiologically relevant ligands: Fibrinogen and iC3b.
Autor:
Alison Rinderspacher, Michael Wyler, Stephan C. Schürer, Yuli Xie, Nathalie Aulner, Dusica Vidovic, Udo Toebben, Lars Branden, Gangli Gong, Yan Feng, Deborah H. Smith, Zhengxiang Zhu, Donald W. Landry, Yidong Liu, Shi Xian Deng, Yufei Tang, Caty Chung
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1191-1194
An IKKbeta inhibitor reported to block NF-kappaB transcriptional activities in Jurkat T cells, was found to enhance NF-kappaB translocation in HUVEC cells. These studies suggested a noncanonical NF-kappaB signaling pathway independent of IKKbeta in H
Autor:
Claudia Ruiz, Michael D. Cameron, Philip LoGrasso, E. Hampton Sessions, Thomas Schröter, Thomas D. Bannister, Evelyn Griffin, Stephan C. Schürer, Jennifer Pocas, Li Lin, Amiee Weiser, Yan Yin, Yangbo Feng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:6390-6393
Inhibitors of Rho kinase have been developed based on two distinct scaffolds, benzimidazoles, and benzoxazoles. SAR studies and efforts to optimize the initial lead compounds are described. Novel selective inhibitors of ROCK-II with excellent potency
Autor:
Maria Laura Cremona, Ai Yamamoto, Udo Többen, Dusica Vidovic, Yuli Xie, Nathalie Aulner, Donald W. Landry, Caty Chung, Lars Branden, Gangli Gong, Katherine M. Myers, Alison Rinderspacher, Stephan C. Schürer, Yidong Liu, Monique Andersen, Shi Xian Deng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1715-1717
A quinazoline that decreases polyglutamine aggregate burden in a cell-based assay was identified from a high-throughput screen of a chemical-compound library, provided by the NIH Molecular Libraries Small Molecule Repository (MLSMR). A structure and
Autor:
Thomas Schröter, Yan Yin, Michael D. Cameron, Stephan C. Schürer, Derek R. Duckett, Wayne Grant, Philip LoGrasso, Claudia Ruiz, Yangbo Feng, Jennifer Pocas, Li Lin, Weimin Chen
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(23)
A series of benzothiazole derivatives as ROCK inhibitors have been discovered. Compounds with good biochemical and cellular potency, and sufficient kinase selectivity have been identified.
Autor:
Christophe Morisseau, Yidong Liu, Fang Yan, Donald W. Landry, Bruce D. Hammock, Caty Chung, Shi Xian Deng, Xiangpo Li, Lars Branden, Gangli Gong, Yan Feng, Deborah H. Smith, Zhengxiang Zhu, Dusica Vidovic, Alison Rinderspacher, Stephan C. Schürer, Yuli Xie
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(8)
Soluble epoxide hydrolase (sEH) is a novel target for the treatment of hypertension and vascular inflammation. A new class of potent non-urea sEH inhibitors was identified via high throughput screening (HTS) and chemical modification. IC(50)s of the
Autor:
Yen Ting Chen, Michael D. Cameron, Thomas D. Bannister, Evelyn Griffin, Claudia Ruiz, Stephan C. Schürer, Derek R. Duckett, Thomas Schröter, Yangbo Feng, Philip LoGrasso, Li Lin, Amiee Weiser
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(24)
Inhibition of Rho kinase (ROCK) is an attractive strategy for the treatment of diseases such as hypertension, glaucoma, and cancer. Here we report chroman-3-amides as highly potent ROCK inhibitors with sufficient kinase selectivity, excellent cell ac