Synthesis of Highly Substituted Dibenzo[b,f]azocines and Their Evaluation as Protein Kinase Inhibitors

Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee, United States
Bioorganic & Medicinal Chemistry Letters (Impact Factor: 2.42). 11/2006; 16(20):5360-3. DOI: 10.1016/j.bmcl.2006.07.078
Source: PubMed


Synthetic routes towards highly substituted eight membered ring heterocycles fused to aryl rings such as the dibenzo[b,f]azocine system are still lacking. Herein, we present a convenient convergent synthetic route towards this heterocyclic class of compounds with possible variations at positions 4, 7, and 11. One member of a library of dibenzo[b,f]azocines with different substituents at position 11 was identified to inhibit protein kinase A activity (IC50 = 122 mu M) but not protein kinase C. (c) 2006 Elsevier Ltd. All rights reserved.

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