Extended knowledge of 42923-79-5

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 42923-79-5, help many people in the next few years.Formula: C9H10N2O2

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Formula: C9H10N2O2, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 42923-79-5, name is 7-Nitro-1,2,3,4-tetrahydroisoquinoline. In an article£¬Which mentioned a new discovery about 42923-79-5

3-(3,4-dihydroisoquinolin-2(1 H)-ylsulfonyl)benzoic acids: Highly potent and selective inhibitors of the type 5 17-beta-hydroxysteroid dehydrogenase AKR1C3

A high-throughput screen identified 3-(3,4-dihydroisoquinolin-2(1H)- ylsulfonyl)benzoic acid as a novel, highly potent (low nM), and isoform-selective (1500-fold) inhibitor of aldo-keto reductase AKR1C3: a target of interest in both breast and prostate cancer. Crystal structure studies showed that the carboxylate group occupies the oxyanion hole in the enzyme, while the sulfonamide provides the correct twist to allow the dihydroisoquinoline to bind in an adjacent hydrophobic pocket. SAR studies around this lead showed that the positioning of the carboxylate was critical, although it could be substituted by acid isosteres and amides. Small substituents on the dihydroisoquinoline gave improvements in potency. A set of “reverse sulfonamides” showed a 12-fold preference for the R stereoisomer. The compounds showed good cellular potency, as measured by inhibition of AKR1C3 metabolism of a known dinitrobenzamide substrate, with a broad rank order between enzymic and cellular activity, but amide analogues were more effective than predicted by the cellular assay.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 42923-79-5, help many people in the next few years.Formula: C9H10N2O2

Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem