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  • Title: Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable.
    Author: Buttar D, Edge M, Emery SC, Fitzek M, Forder C, Griffen A, Hayter B, Hayward CF, Hopcroft PJ, Luke RW, Page K, Stawpert J, Wright A.
    Journal: Bioorg Med Chem Lett; 2008 Aug 15; 18(16):4723-6. PubMed ID: 18676144.
    Abstract:
    Tie-2 is a receptor tyrosine kinase which is involved in angiogenesis and thereby growth of human tumours. The discovery and SAR of a novel class of imidazole-vinyl-pyrimidine kinase inhibitors, which inhibit Tie-2 in vitro is reported. Their synthesis was carried out by condensation of imidazole aldehydes with methyl pyrimidines. These compounds are lead-like, with low molecular weight, good physical properties and oral bioavailability.
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