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Synthesis and structure–activity relationship of 2-arylamino-4-aryl-pyrimidines as potent PAK1 inhibitors

DOI: 10.1016/j.bmcl.2013.05.059
Title: Synthesis and structure–activity relationship of 2-arylamino-4-aryl-pyrimidines as potent PAK1 inhibitors
Journal Title: Bioorganic & Medicinal Chemistry Letters
Volume: 23
Issue: 14
Publication Date: 15 July 2013
Start Page: 4072
End Page: 4075
Published online: online 28 May 2013
ISSN: 0960-894X
Affiliations:
  • Astex Pharmaceuticals, Inc., 4140 Dublin Boulevard, Suite 200, Dublin, CA 94568, USA
  • Abstract: ino-4-aryl-pyrimidines were found to be potent inhibitors of PAK1 kinase. The Synthesis and SAR are described. The incorporation of a bromide at the 5-position of the pyrimidine core and in combination with a 1,2-dimethylpiperazine pendant domain yielded a lead compound with potent PAK1 inhibition and anti-proliferative activity in various colon cancer cell lines.
    Accepted: 17 May 2013
    Received: 14 March 2013
    Revised: 13 May 2013
    Keywords: PAK1 kinase; 2-Arylamino-4-aryl-pyrimidines; Colon cancer; Pak1 inhibitor; Bioisostere
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