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Identification of a novel class of selective Tpl2 kinase inhibitors: 4-Alkylamino-[1,7]naphthyridine-3-carbonitriles

Autor: Jennifer R. Thomason, J. Perry Hall, Kristin Janz, Huan-Qiu Li, Lori Krim Gavrin, Jean-Baptiste Telliez, Lih-Ling Lin, Neelu Kaila, John W. Cuozzo, Sang Hsu, Neal Green, Tam Steve Yik-Kai, Qin Wang, Yonghan Hu, Cheryl Nickerson-Nutter, Dennis Powell

Publikováno v: Bioorganic & Medicinal Chemistry. 15:6425-6442

We have previously reported the discovery and initial SAR of the [1,7]naphthyridine-3-carbonitriles and quinoline-3-carbonitriles as Tumor Progression Loci-2 (Tpl2) kinase inhibitors. In this paper, we report new SAR efforts which have led to the ide

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::31906fb62238856f248cf9b5ac3ff088
https://doi.org/10.1016/j.bmc.2007.06.054

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Inhibition of Tpl2 kinase and TNFα production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis

Autor: Jean-Baptiste Telliez, Tam Steve Yik-Kai, Neal Green, Huan-Qiu Li, Yonghan Hu, Cheryl Nickerson-Nutter, Neelu Kaila, Lori Krim Gavrin, Jennifer R. Thomason, J. Perry Hall, John W. Cuozzo, Sang Hsu, Kristin Janz, Lih-Ling Lin

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:6067-6072

The synthesis and structure-activity studies of a series of quinoline-3-carbonitriles as inhibitors of Tpl2 kinase are described. Potent inhibitors of Tpl2 kinase with selectivity against a panel of selected kinases in enzymatic assays and specificit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69b8e72dbb3c6462e2e9e6c26baea191
https://doi.org/10.1016/j.bmcl.2006.08.102

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Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure–activity relationships

Autor: Neelu Kaila, Neal Green, Huan-Qiu Li, Yonghan Hu, Jennifer R. Thomason, J. Perry Hall, Ariamala Gopalsamy, Tam Steve Yik-Kai, Kristin Janz, Lih-Ling Lin, Greg Ciszewski, Jean-Baptiste Telliez, Lori Krim Gavrin, John W. Cuozzo, Sang Hsu

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 15:5288-5292

The synthesis and structure-activity studies of a series of 6-substituted-4-anilino-[1,7]-naphthyridine-3-carbonitriles as inhibitors of Tpl2 kinase are described. The early exploratory work described here may lead to the discovery of compounds with

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aae56440af2384540091d86613ec70fd
https://doi.org/10.1016/j.bmcl.2005.08.029

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Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood

Autor: Neal Green, Lih-Ling Lin, J. Perry Hall, G. Roger Askew, Katherine J. Seidl, Tam Steve Yik-Kai, James D. Clark, Yonghan Hu, Jean-Baptiste Telliez, John W. Cuozzo, Sang Hsu, Aaron Winkler, Yahya Kurdi, Julie Liu

Publikováno v: The Journal of biological chemistry. 282(46)

Tumor necrosis factor alpha (TNFalpha) is a pro-inflammatory cytokine that controls the initiation and progression of inflammatory diseases such as rheumatoid arthritis. Tpl2 is a MAPKKK in the MAPK (i.e. ERK) pathway, and the Tpl2-MEK-ERK signaling

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e5eadac314a1eb8f1e36a24b92d3647c
https://pubmed.ncbi.nlm.nih.gov/17848581

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A rat pharmacokinetic/pharmacodynamic model for assessment of lipopolysaccharide-induced tumor necrosis factor-alpha production

Autor: Jeremy I. Levin, Qin Wang, Xin Xu, Neal Green, Vikram Patel, Nevena Mollova, Shannon Chesley, John W. Cuozzo, Yuhua Zhang, Uma Raut, Lih-Ling Lin, J. Perry Hall

Publikováno v: Journal of pharmacological and toxicological methods. 56(1)

Introduction Tumor necrosis factor-alpha (TNFα) participates in many inflammatory processes. TNFα modulators show beneficial effects for the treatment of many diseases including rheumatoid arthritis. The purpose of this study was to validate a rat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d62edece02a660bc5ff87c06f099d677
https://pubmed.ncbi.nlm.nih.gov/17391989

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Structure-activity studies of a series of dipyrazolo[3,4-b:3',4'-d]pyridin-3-ones binding to the immune regulatory protein B7.1

Autor: Lihren Chen, Jing Chen, Jason Shaoyun Xiang, Dave Erbe, Audrey Molina Davies, Neal Green, James Tobin, Tam Steve Yik-Kai

Publikováno v: Bioorganicmedicinal chemistry. 11(13)

The interaction of co-stimulatory molecules on T cells with B7 molecules on antigen presenting cells plays an important role in the activation of naive T cells. Consequently, agents that disrupt these interactions should have applications in treatmen

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6bfcb1496e700eb98308e8ba51e663de
https://pubmed.ncbi.nlm.nih.gov/12788368

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