Literature DB >> 10698440

The discovery of potent cRaf1 kinase inhibitors.

K Lackey1, M Cory, R Davis, S V Frye, P A Harris, R N Hunter, D K Jung, O B McDonald, R W McNutt, M R Peel, R D Rutkowske, J M Veal, E R Wood.   

Abstract

A series of benzylidene-1H-indol-2-one (oxindole) derivatives was synthesized and evaluated as cRaf-1 kinase inhibitors. The key features of the molecules were the donor/acceptor motif common to kinase inhibitors and a critical acidic phenol flanked by two substitutions. Diverse 5-position substitutions provided compounds with low nanomolar kinase enzyme inhibition and inhibited the intracellular MAPK pathway.

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Year:  2000        PMID: 10698440     DOI: 10.1016/s0960-894x(99)00668-x

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


  60 in total

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9.  Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.

Authors:  James Tsai; John T Lee; Weiru Wang; Jiazhong Zhang; Hanna Cho; Shumeye Mamo; Ryan Bremer; Sam Gillette; Jun Kong; Nikolas K Haass; Katrin Sproesser; Ling Li; Keiran S M Smalley; Daniel Fong; Yong-Liang Zhu; Adhirai Marimuthu; Hoa Nguyen; Billy Lam; Jennifer Liu; Ivana Cheung; Julie Rice; Yoshihisa Suzuki; Catherine Luu; Calvin Settachatgul; Rafe Shellooe; John Cantwell; Sung-Hou Kim; Joseph Schlessinger; Kam Y J Zhang; Brian L West; Ben Powell; Gaston Habets; Chao Zhang; Prabha N Ibrahim; Peter Hirth; Dean R Artis; Meenhard Herlyn; Gideon Bollag
Journal:  Proc Natl Acad Sci U S A       Date:  2008-02-19       Impact factor: 11.205

10.  Fluorescent cascade and direct assays for characterization of RAF signaling pathway inhibitors.

Authors:  Kevin R Kupcho; Rica Bruinsma; Tina M Hallis; David A Lasky; Richard L Somberg; Tammy Turek-Etienne; Kurt W Vogel; Kristin G Huwiler
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