Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Jan Lundström"'
Autor:
Zhijun Wang, Erik Boman, Jan Urban, Jeff Kucharski, Hiroshi Nakanishi, Jan Lundström, Nancy G. J. Delaet, Justin T. Ernst, Eddine Saiah, Christopher Lum, Eric Erb, Antonio Garrido Montalban, Susana Conde Ceide, Russell Dahl, Linda Kessler, Stephen E. Miller, Christopher J. Larson, Chau-Dung Chang, Edward Roberts, Jeffrey Kahl, Robert K. P. Sullivan, Andrew Gibbs, David Dalesandro
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4819-4824
We have optimized a novel series of potent p38 MAP kinase inhibitors based on an alpha-ketoamide scaffold through structure based design that due to their extended molecular architecture bind, in addition to the ATP site, to an allosteric pocket. In
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::646db32d2692e24d80d296daacfeccd7
https://doi.org/10.1016/j.bmcl.2010.06.102
https://doi.org/10.1016/j.bmcl.2010.06.102
Autor:
Jan Lundström, Eric Erb, Susana Conde Ceide, Eddine Saiah, Jeff Kahl, Stephen E. Miller, Andrew Gibbs, Edward Roberts, Nancy G. J. Delaet, Antonio Garrido Montalban, Robert K. P. Sullivan, Erik Boman, Zhijun Wang, Christopher J. Larson, David Dalesandro, Russell Dahl, Chau-Dung Chang, Hiroshi Nakanishi, Linda Kessler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5456-5459
We have identified a second series of potent p38 inhibitors. As with our first generation series, these compounds are based on an alpha-ketoamide scaffold. The reversal of the ketoamide order, however, introduces more chemical flexibility and in addi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df8879f4a8eb58917957fc3b2d5d8d5e
https://doi.org/10.1016/j.bmcl.2008.09.028
https://doi.org/10.1016/j.bmcl.2008.09.028
Autor:
Jeff Kucharski, Zhijun Wang, Christopher Lum, Linda Kessler, Jan Lundström, Stephen E. Miller, Robert Sullivan, Edward Roberts, Lubomir Sebo, Yazhong Pei, Hiroshi Nakanishi, Jeff Kahl, Kent Pryor, Jan Urban
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3578-3581
The discovery of two classes of pyrimidine-based inhibitors of GSK-3 is described. Optimization of these series led to inhibitors with IC50 100-fold selectivity over Aurora A kinase. A proposed binding mode of 21b is presented. One compound (33) of t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9152e41d192b1f500eacab1ffb6c04cd
https://doi.org/10.1016/j.bmcl.2008.05.001
https://doi.org/10.1016/j.bmcl.2008.05.001
Autor:
Eric Erb, Russell Dahl, Jan Lundström, Robert K. P. Sullivan, Chau-Dung Chang, Erik Boman, Edward Roberts, Antonio Garrido Montalban, Andrew Gibbs, Justin T. Ernst, Jeffrey Kahl, Hiroshi Nakanishi, Nancy G. J. Delaet, Eddine Saiah, Linda Kessler, Stephen E. Miller, Susana Conde Ceide, Christopher J. Larson, David Dalesandro, Zhijun Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1772-1777
We have identified a novel series of potent p38 MAP kinase inhibitors through structure-based design which due to their extended molecular architecture bind, in addition to the ATP site, to an allosteric pocket. In vitro ADME and in vivo PK studies s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e1a60a704c68cbb7566ac6bd4230098
https://doi.org/10.1016/j.bmcl.2008.02.033
https://doi.org/10.1016/j.bmcl.2008.02.033
Publikováno v:
European Journal of Pharmacology. 386:15-24
In the kynurenine pathway of tryptophan metabolism, 3-hydroxyanthranilic acid is the substrate for formation of the excitotoxin quinolinic acid by 3-hydroxyanthranilic acid 3,4-dioxygenase. This study was designed to characterize the effects on 3-hyd
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aef47f9711a754cb9afa88890dec932f
https://doi.org/10.1016/s0014-2999(99)00683-4
https://doi.org/10.1016/s0014-2999(99)00683-4
Publikováno v:
European Journal of Pharmaceutical Sciences. 5:199-208
Due to its highly ionic nature, the antiviral phosphonoformate shows poor penetration into cells and here bioreversible prodrugs of phosphonoformate are designed in an attempt to improve its transport properties. The key step in the syntheses of tri[
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::16cca19a76f52b6166ae0782d41a5d1a
https://doi.org/10.1016/s0928-0987(97)00281-9
https://doi.org/10.1016/s0928-0987(97)00281-9
Publikováno v:
Tetrahedron. 52:14937-14950
Sodium pivaloyloxymethyl (pivaloyloxymethoxycarbonyl)phosphonate 4 , sodium 4-acyloxybenzyl phenoxycarbonylphosphonates 14a-c and sodium 4-acyloxybenzyl benzyloxycarbonylphosphonates 15a,b have been prepared as bioreversible prodrugs of the antiviral
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3a28ea1652f978f163af29fb591013d2
https://doi.org/10.1016/0040-4020(96)00906-4
https://doi.org/10.1016/0040-4020(96)00906-4
Autor:
J.-O. Svensson, T. Hansson, Jan Lundström, C. Von Bahr, Magnus Ingelman-Sundberg, M. Marklund
Publikováno v:
Pharmacology & Toxicology. 71:416-419
Incubation of the tricyclic antidepressant desmethylimpramine (DMI) with rat liver or brain microsomes in the presence of NADPH or t-butyl-hydroperoxide (TBH) revealed different regiospecificities in the hydroxylation reactions between the tissues. I
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ecd488f04a45a56af70202b7e91c3c3b
https://doi.org/10.1111/j.1600-0773.1992.tb00571.x
https://doi.org/10.1111/j.1600-0773.1992.tb00571.x
Autor:
David Dalesandro, Eddine Saiah, Antonio Garrido Montalban, Justin T. Ernst, Stephen E. Miller, Christopher J. Larson, Hiroshi Nakanishi, Russell Dahl, Eric Erb, Edward Roberts, Zhijun Wang, Susana Conde Ceide, Linda Kessler, Jeffrey Kahl, Andrew Gibbs, Erik Boman, Robert K. P. Sullivan, Nancy G. J. Delaet, Chau-Dung Chang, Jan Lundström
Publikováno v:
European journal of pharmacology. 632(1-3)
The tumor necrosis factor-alpha (TNF-alpha) cytokine, secreted by activated monocytes/macrophages and T lymphocytes, is implicated in several diseases, including rheumatoid arthritis, chronic obstructive pulmonary disease, inflammatory bowel disease,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::84966429599745c5e41120e6e036f2b6
https://pubmed.ncbi.nlm.nih.gov/20132813
https://pubmed.ncbi.nlm.nih.gov/20132813
Autor:
Miller Stephen, Lubomir Sebo, Justin T. Ernst, Russell Dahl, Christopher Lum, Jan Urban, Jan Lundström
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(4)
A novel series of imidazopiperidine-tropane CCR5 antagonists is described. The series was optimized for anti-HIV-1 potency using a set of phenotypic viral entry assays. This strategy resulted in the identification of several very potent (IC 50 < 10 n
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6e67ebea0bfc7e651957180ca090e01e
https://pubmed.ncbi.nlm.nih.gov/18194864
https://pubmed.ncbi.nlm.nih.gov/18194864