Literature DB >> 19362830

Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.

Ariamala Gopalsamy1, Greg Ciszewski, Yongbo Hu, Frederick Lee, Larry Feldberg, Eileen Frommer, Steven Kim, Karen Collins, Donald Wojciechowicz, Robert Mallon.   

Abstract

B-Raf kinase plays a critical role in the Raf-MEK-ERK signaling pathway and inhibitors of B-Raf could be used in the treatment of melanomas, colorectal cancer, and other Ras related human cancers. We have identified novel small molecule pyrazolo[1,5-a]pyrimidine derivatives as B-Raf kinase inhibitors. Structure-activity relationship was generated for various regions of the scaffold to improve the biochemical profile.

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Year:  2009        PMID: 19362830     DOI: 10.1016/j.bmcl.2009.03.129

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


  2 in total

1.  Design, Synthesis and Antitumor Evaluation of Novel Pyrazolopyrimidines and Pyrazoloquinazolines.

Authors:  Mohamed El-Naggar; Ashraf S Hassan; Hanem M Awad; Mohamed F Mady
Journal:  Molecules       Date:  2018-05-23       Impact factor: 4.411

Review 2.  In silico Methods for Design of Kinase Inhibitors as Anticancer Drugs.

Authors:  Zarko Gagic; Dusan Ruzic; Nemanja Djokovic; Teodora Djikic; Katarina Nikolic
Journal:  Front Chem       Date:  2020-01-08       Impact factor: 5.221

  2 in total

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