Literature DB >> 12729639

2,4-disubstituted pyrimidines: a novel class of KDR kinase inhibitors.

Peter J Manley1, Adrienne E Balitza, Mark T Bilodeau, Kathleen E Coll, George D Hartman, Rosemary C McFall, Keith W Rickert, Leonard D Rodman, Kenneth A Thomas.   

Abstract

2,4-Disubstituted pyrimidines were synthesized as a novel class of KDR kinase inhibitors. Evaluation of the SAR of the screening lead compound 1 (KDR IC(50)=105 nM, Cell IC(50)=8% inhibition at 500 nM) led to the potent 3,5-dimethylaniline derivative 2d (KDR IC(50)=6 nM, cell IC(50)=19 nM).

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Year:  2003        PMID: 12729639     DOI: 10.1016/s0960-894x(03)00244-0

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


  1 in total

1.  Expanding the diversity of allosteric bcr-abl inhibitors.

Authors:  Xianming Deng; Barun Okram; Qiang Ding; Jianming Zhang; Yongmun Choi; Francisco J Adrián; Amy Wojciechowski; Guobao Zhang; Jianwei Che; Badry Bursulaya; Sandra W Cowan-Jacob; Gabriele Rummel; Taebo Sim; Nathanael S Gray
Journal:  J Med Chem       Date:  2010-10-14       Impact factor: 7.446

  1 in total

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