• Bioorg. Med. Chem. Lett. · May 2013

    Discovery and synthesis of novel 4-aminopyrrolopyrimidine Tie-2 kinase inhibitors for the treatment of solid tumors.

    • Joel T Arcari, Jean S Beebe, Martin A Berliner, Vincent Bernardo, Merin Boehm, Gary V Borzillo, Tracey Clark, Bruce D Cohen, Richard D Connell, Heather N Frost, Deborah A Gordon, William M Hungerford, Shefali M Kakar, Aaron Kanter, Nandell F Keene, Elizabeth A Knauth, Susan D Lagreca, Yong Lu, Louis Martinez-Alsina, Matthew A Marx, Joel Morris, Nandini C Patel, Doug Savage, Cathy I Soderstrom, Carl Thompson, George Tkalcevic, Norma J Tom, Felix F Vajdos, James J Valentine, Patrick W Vincent, Matthew D Wessel, and Jinshan M Chen.
    • Worldwide Research and Development, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States.
    • Bioorg. Med. Chem. Lett. 2013 May 15; 23 (10): 3059-63.

    AbstractThe synthesis and biological evaluation of novel Tie-2 kinase inhibitors are presented. Based on the pyrrolopyrimidine chemotype, several new series are described, including the benzimidazole series by linking a benzimidazole to the C5-position of the 4-amino-pyrrolopyrimidine core and the ketophenyl series synthesized by incorporating a ketophenyl group to the C5-position. Medicinal chemistry efforts led to potent Tie-2 inhibitors. Compound 15, a ketophenyl pyrrolopyrimidine urea analog with improved physicochemical properties, demonstrated favorable in vitro attributes as well as dose responsive and robust oral tumor growth inhibition in animal models.Copyright © 2013 Elsevier Ltd. All rights reserved.

      Pubmed     Full text   Copy Citation     Plaintext  

      Add institutional full text...

    Notes

     
    Knowledge, pearl, summary or comment to share?
    300 characters remaining
    help        
    You can also include formatting, links, images and footnotes in your notes
    • Simple formatting can be added to notes, such as *italics*, _underline_ or **bold**.
    • Superscript can be denoted by <sup>text</sup> and subscript <sub>text</sub>.
    • Numbered or bulleted lists can be created using either numbered lines 1. 2. 3., hyphens - or asterisks *.
    • Links can be included with: [my link to pubmed](http://pubmed.com)
    • Images can be included with: ![alt text](https://bestmedicaljournal.com/study_graph.jpg "Image Title Text")
    • For footnotes use [^1](This is a footnote.) inline.
    • Or use an inline reference [^1] to refer to a longer footnote elseweher in the document [^1]: This is a long footnote..

    hide…