Literature DB >> 19762237

First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors.

Chuansheng Niu1, Diane H Boschelli, L Nathan Tumey, Niala Bhagirath, Joan Subrath, Jaechul Shim, Yan Wang, Biqi Wu, Clark Eid, Julie Lee, Xiaoke Yang, Agnes Brennan, Divya Chaudhary.   

Abstract

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.

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Year:  2009        PMID: 19762237     DOI: 10.1016/j.bmcl.2009.08.086

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway.

Authors:  Celeste Alverez; Stacie L Bulfer; Ramappa Chakrasali; Michael S Chimenti; Raymond J Deshaies; Neal Green; Mark Kelly; Matthew G LaPorte; Taber S Lewis; Mary Liang; William J Moore; R Jeffrey Neitz; Vsevolod A Peshkov; Michael A Walters; Feng Zhang; Michelle R Arkin; Peter Wipf; Donna M Huryn
Journal:  ACS Med Chem Lett       Date:  2015-12-22       Impact factor: 4.345

2.  Prediction of PKCθ inhibitory activity using the Random Forest Algorithm.

Authors:  Ming Hao; Yan Li; Yonghua Wang; Shuwei Zhang
Journal:  Int J Mol Sci       Date:  2010-09-20       Impact factor: 5.923

Review 3.  The Novel PKCθ from Benchtop to Clinic.

Authors:  Rouba Hage-Sleiman; Asmaa B Hamze; Lina Reslan; Hadile Kobeissy; Ghassan Dbaibo
Journal:  J Immunol Res       Date:  2015-05-19       Impact factor: 4.818

  3 in total

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