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  • Title: Novel tricyclic azepine derivatives: Biological evaluation of pyrimido[4,5-b]-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase.
    Author: Smith L, Wong WC, Kiselyov AS, Burdzovic-Wizemann S, Mao Y, Xu Y, Duncton MA, Kim K, Piatnitski EL, Doody JF, Wang Y, Rosler RL, Milligan D, Columbus J, Balagtas C, Lee SP, Konovalov A, Hadari YR.
    Journal: Bioorg Med Chem Lett; 2006 Oct 01; 16(19):5102-6. PubMed ID: 16887347.
    Abstract:
    Novel tricyclic derivatives containing an oxazepine, thiazepine, or diazepine ring were studied for their EGFR tyrosine kinase inhibitory activity. While the oxazepines were in general more potent than thiazepines, the diazepines displayed somewhat different structure-activity relationships. Moreover, the diazepines, in contrast to the oxazepines, showed appreciable inhibitory activity against the KDR tyrosine kinase. Furthermore, both oxazepines and diazepines demonstrated significant ability to inhibit autophosphorylation of EGFR in DiFi cells (generally, IC(50) values in the single-digit micromolar to submicromolar range).
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