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SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase
  • B. Bennett, D. Sasaki, +10 authors David W. Anderson
  • Biology, Medicine
  • Proceedings of the National Academy of Sciences…
  • 20 November 2001
TLDR
SP600125 blocked (bacterial) lipopolysaccharide-induced expression of tumor necrosis factor-α and inhibited anti-CD3-induced apoptosis of CD4+ CD8+ thymocytes and supports targeting JNK as an important strategy in inflammatory disease, apoptotic cell death, and cancer. Expand
JNK mediates hepatic ischemia reperfusion injury.
TLDR
JNK inhibition transiently blocks phosphorylation of c-Jun at an early time point after reperfusion, and AP-1 activation is also substantially blocked, suggesting that JNK activity induces cell death by both pathways. Expand
Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.
TLDR
Crystallography studies suggest that the 2-substituent may have a conformational effect favoring the extended binding conformation inhibitors based on the benzimidazole scaffold. Expand
Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors.
TLDR
Investigation of a hit from high-throughput screening identified a series of thiophene-substituted anthranilamides as potent nonamidine fXa inhibitors as well as compounds with picomolar inhibitory potency and micromolar in vitro anticoagulant activity. Expand
Discovery and optimization of thieno[2,3-d]pyrimidines as B-Raf inhibitors.
TLDR
Thieno[2,3-d]pyrimidines is identified as a core scaffold of small molecule B-Raf inhibitors and the SAR of analogs in this series will be described. Expand
Chemically modified dansyl probes: a fluorescent diagnostic for ion and proton detection in solution and in polymers.
TLDR
Addition of acids and metal ions to solutions of trimethylethylenediamine naphthalene sulfonamide (trinsyl) 2 produces a >25-fold increase in fluorescence intensity. Expand
Substituted thiophene-anthranilamides as potent inhibitors of human factor Xa.
A series of thiophene-containing non-amidine factor Xa inhibitors is described. Simple methyl-substituted thiophene analogs were relatively weak inhibitors. However, introduction of hydrophilicExpand
Bridged to Fused Ring Interchange. Methodology for the Construction of Fused Cycloheptanes and Cyclooctanes. Total Syntheses of Ledol, Ledene, and Compressanolide.
TLDR
The T2IMDA provides a synthesis for rigid bridged bicyclic molecules that can be stereoselectively elaborated before ozonolysis of the bridgehead double bond and is amenable to the synthesis of terpene natural products. Expand
Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity.
TLDR
Substitution of a nitro group at the 4-position on the benzimidazole improves both potency against fXa and selectivity versus thrombin and replace of the naphthylamidine group with either a biphenylamidine or propenylbenzamidine. Expand
Design and synthesis of aminophenol-based factor Xa inhibitors.
TLDR
A novel potent and selective aminophenol scaffold for fXa inhibitors was developed from a previously reported benzimidazole-based naphthylamidine template, which produced selective, sub-nanomolar f Xa inhibitors. Expand
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