geoscience.net logo
+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors


, : First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors. Bioorganic & Medicinal Chemistry Letters 19(20): 5829-5832

A series of 5-vinyl-3-pyridinecarbonitriles were synthesized and evaluated as PKCtheta inhibitors. The systematic optimization of 4-[(4-methyl-1H-indol-5-yl)amino]-5-[(E)-2-phenylvinyl]-3-pyridinecarbonitrile 3 resulted in the identification of compound 23e as a potent PKCtheta inhibitor with good selectivity over PKCdelta.

US$19.90

PMID: 19762237

DOI: 10.1016/j.bmcl.2009.08.086


Other references

Aizawa, H.; Kozima, S.; Takagi, A., 1989: Ultrasound imaging of muscles in Duchenne muscular dystrophy. The ultrasound imaging of quadriceps, gastrocnemius and soleus muscles was performed in 30 patients with Duchenne muscular dystrophy (DMD) and 16 control subjects. In controls, the skeletal muscle itself was scarcely echogenic. However, bone surfa...

Donnini, G., 1955: The reductase test for the evaluation of milk I Principles, technic and degree of accuracy A review. Giorn Batteriol E Immunol10: 406-438

Gibson F., 1971: Tyrosine and phenyl alanine biosynthesis the t and p proteins aerobacter aerogenes chorismate mutase pisum sativum d. Tabor, Herbert And Celia White Tabor (edited By)ds In Enzymology, Vol. Xvii. Metabolism Of Amino Acids And Amines. Xxxi 1098p. Illus. Aca Demic Press: New York, N.y., U.s.a.; London, England. . 564-574

Sturgeon R.J.; Schulman S.G., 1980: The reaction of doxorubicin and dna at high nucleotide to drug ratios. The interactions of the monocation of the antitumor, anthracycline antibiotic doxorubicin with calf thymus DNA were studied. In the intercalative region, with high DNA phosphate to cation ratios, the drug is sequestered by 4 phosphate groups. A no...

Baxter, D.A.; Byrne, J.H., 1990: Reduction of voltage-activated K+ currents by forskolin is not mediated via cAMP in pleural sensory neurons of Aplysia. 1. Forskolin is often used to activate adenylate cyclase in studies relating adenosine 3',5'-cyclic monophosphate (cAMP) to the modulation of membrane current. There is growing concern, however, that some actions of forskolin are indepen...

Ala-Pietilä, P., 2002: Towards personal communication technology and health care. Duodecim; Laaketieteellinen Aikakauskirja 117(23): 2343-2345

Anonymous, 2012: The p53 inhibitor pifithrin-alpha can stimulate fibrosis in a rat model of ischemic acute kidney injury. Inhibition of the tumor suppressor p53 diminishes tubular cell apoptosis and protects renal function in animal models of acute kidney injury (AKI). Therefore, targeting p53 has become an attractive therapeutic strategy in the approach to AKI. Alth...

Butler, J.; Obermiller, T.; Willoughby, S.; Lakshminarayan, S., 1990: Reflux pulmonary vein flow prevents pulmonary infarction after pulmonary artery obstruction. Küttner showed in 1874 that simultaneous ligation of the pulmonary veins increased the frequency and severity of lung infarctions after pulmonary artery obstruction. The authors studied the possibility that a tidal pulmonary venous blood flow ref...

Lammert, A.; Goldstein, L.; Ramanarayanan, V.; Narayanan, S., 2016: Gestural Control in the English Past-Tense Suffix: An Articulatory Study Using Real-Time MRI. The English past tense allomorph following a coronal stop (e.g., /bɑndəd/) includes a vocoid that has traditionally been transcribed as a schwa or as a barred i. Previous evidence has suggested that this entity does not involve a specific articu...

Grillo, M.A.; Li, C.; Fowlkes, A.M.; Briggeman, T.M.; Zhou, A.; Schemske, D.W.; Sang, T., 2009: Genetic architecture for the adaptive origin of annual wild rice, oryza nivara. The wild progenitors of cultivated rice, Oryza nivara and Oryza rufipogon, provide an experimental system for characterizing the genetic basis of adaptation. The evolution of annual O. nivara from a perennial ancestor resembling its sister species...