Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.
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Buchanan JL, Newcomb JR, Carney DP, Chaffee SC, Chai L, Cupples R, Epstein LF, Gallant P, Gu Y, Harmange JC, Hodge K, Houk BE, Huang X, Jona J, Joseph S, Jun HT, Kumar R, Li C, Lu J, Menges T, Morrison MJ, Novak PM, van der Plas S, Radinsky R, Rose PE, Sawant S, Sun JR, Surapaneni S, Turci SM, Xu K, Yanez E, Zhao H, Zhu X
Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.
Bioorg Med Chem Lett. 2011 Apr 15;21(8):2394-9. doi: 10.1016/j.bmcl.2011.02.075. Epub 2011 Feb 23.
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- 21414779 [ View in PubMed]
- Abstract
The insulin-like growth factor-1 receptor (IGF-1R) plays an important role in the regulation of cell growth and differentiation, and in protection from apoptosis. IGF-1R has been shown to be an appealing target for the treatment of human cancer. Herein, we report the synthesis, structure-activity relationships (SAR), X-ray cocrystal structure and in vivo tumor study results for a series of 2,4-bis-arylamino-1,3-pyrimidines.