188781-43-3Relevant articles and documents
Reaction of nitroorganic compounds using thiourea catalysts anchored to polymer support
Miyabe, Hideto,Tuchida, Sayo,Yamauchi, Masashige,Takemoto, Yoshiji
, p. 3295 - 3300 (2008/09/17)
Immobilization of chiral thiourea catalyst was studied. The PEG-bound thiourea showed better catalytic activity than those of the carboxypolystyrene HL resin-bound and TentaGel carboxy resin-bound thioureas. In the presence of PEG-bound thiourea, Michael and tandem Michael reactions of trans-β- nitrostyrene proceeded enantioselectively. Georg Thieme Verlag Stuttgart.
2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3',5'- bis(trifluoromethyl)phenyl)carboxamide: A potent inhibitor of NF-κB- and AP- 1-mediated gene expression identified using solution-phase combinatorial chemistry
Sullivan, Robert W.,Bigam, Colin G.,Erdman, Paul E.,Palanki, Moorthy S. S.,Anderson, David W.,Goldman, Mark E.,Ransone, Lynn J.,Suto, Mark J.
, p. 413 - 419 (2007/10/03)
Described is the identification of a novel series of compounds that blocks the activation of two key transcription factors, AP-1 and NF-κB. These transcription factors regulate the expression of several critical proinflammatory proteins and cytokines and represent attractive targets for drug discovery. Through the use of high throughput screening and solution- phase parallel synthesis, inhibitors of both NF-κB and AP-1 were identified. In subsequent testing, these compounds were also shown to block both IL-2 and IL-8 levels in the same cells. One of the most potent compounds in this series, 28, was active in several animal models of inflammation and immunosuppression, thus validating the importance of AP-1 and NF-κB as potential therapeutic targets. The synthesis and preliminary structure- activity relationships of these compounds is addressed.
