Murray, Jeremy M.; Sweeney, Zachary K.; Chan, Bryan K.; Balazs, Mercedesz; Bradley, Erin; Castanedo, Georgette; Chabot, Christine; Chantry, David; Flagella, Michael; Goldstein, David M.; Kondru, Rama; Lesnick, John; Li, Jun; Lucas, Matthew C.; Nonomiya, Jim; Pang, Jodie; Price, Stephen; Salphati, Laurent; Safina, Brian; Savy, Pascal P. A.; Seward, Eileen M.; Ultsch, Mark; Sutherlin, Daniel P. published the artcile< Potent and Highly Selective Benzimidazole Inhibitors of PI3-Kinase Delta>, Product Details of C6H4Cl2N4, the main research area is benzimidazole preparation PI3 kinase inhibitor SAR.
Inhibition of PI3Kδ is considered to be an attractive mechanism for the treatment of inflammatory diseases and leukocyte malignancies. Using a structure-based design approach, we have identified a series of potent and selective benzimidazole-based inhibitors of PI3Kδ. These inhibitors do not occupy the selectivity pocket between Trp760 and Met752 that is induced by other families of PI3Kδ inhibitors. Instead, the selectivity of the compounds for inhibition of PI3Kδ relative to other PI3K isoforms appears to be due primarily to the strong interactions these inhibitors are able to make with Trp760 in the PI3Kδ binding pocket. The pharmacokinetic properties and the ability of compound 5 (I) to inhibit the function of B-cells in vivo are described.
Journal of Medicinal Chemistry published new progress about Anti-inflammatory agents. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Product Details of C6H4Cl2N4.
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