Knight, Zachary A. published the artcileIsoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold, Recommanded Product: 3-Morpholinophenol, the publication is Bioorganic & Medicinal Chemistry (2004), 12(17), 4749-4759, database is CAplus and MEDLINE.
Phosphoinositide 3-kinases (PI3-Ks) are an ubiquitous class of signaling enzymes that regulate diverse cellular processes including growth, differentiation, and motility. Physiol. roles of PI3-Ks have traditionally been assigned using two pharmacol. inhibitors, LY294002 and wortmannin. Although these compounds are broadly specific for the PI3-K family, they show little selectivity among family members, and the development of isoform-specific inhibitors of these enzymes has been long anticipated. Herein, the preparation of two classes of arylmorpholine PI3-K inhibitors and the characterization of their specificity against a comprehensive panel of targets within the PI3-K family are reported. Multiplex inhibitors that potently inhibit distinct subsets of PI3-K isoforms, including the first selective inhibitor of p110β/p110δ (IC50 p110β = 0.13 μM, p110δ = 0.63 μM), were identified. Trends that suggest certain PI3-K isoforms may be more sensitive to potent inhibition by arylmorpholines, thereby guiding future drug design based on this pharmacophore, were also identified.
Bioorganic & Medicinal Chemistry published new progress about 27292-49-5. 27292-49-5 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Benzene,Phenol, name is 3-Morpholinophenol, and the molecular formula is C10H13NO2, Recommanded Product: 3-Morpholinophenol.
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