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Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.
Buchanan, John L; Newcomb, John R; Carney, David P; Chaffee, Stuart C; Chai, Lilly; Cupples, Rod; Epstein, Linda F; Gallant, Paul; Gu, Yan; Harmange, Jean-Christophe; Hodge, Kathy; Houk, Brett E; Huang, Xin; Jona, Janan; Joseph, Smriti; Jun, H Toni; Kumar, Rakesh; Li, Chun; Lu, John; Menges, Tom; Morrison, Michael J; Novak, Perry M; van der Plas, Simon; Radinsky, Robert; Rose, Paul E; Sawant, Satin; Sun, Ji-Rong; Surapaneni, Sekhar; Turci, Susan M; Xu, Keyang; Yanez, Evelyn; Zhao, Huilin; Zhu, Xiaotian.
Bioorg Med Chem Lett ; 21(8): 2394-9, 2011 Apr 15.
Article in English | MEDLINE | ID: mdl-21414779

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.


Subject(s)
Protein Kinase Inhibitors/chemistry , Pyrimidines/chemistry , Quinolines/chemical synthesis , Receptor, IGF Type 1/antagonists & inhibitors , Animals , Binding Sites , Crystallography, X-Ray , Drug Evaluation, Preclinical , Humans , Mice , Protein Kinase Inhibitors/chemical synthesis , Protein Kinase Inhibitors/pharmacokinetics , Pyrimidines/chemical synthesis , Pyrimidines/pharmacokinetics , Quinolines/chemistry , Quinolines/pharmacokinetics , Receptor, IGF Type 1/metabolism , Structure-Activity Relationship , Xenograft Model Antitumor Assays
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