Targeting the Polyamine Transport System with Benzazepine-and Azepine-Polyamine Conjugates†

…, V Cerec, M Le Roch, P Uriac, JG Delcros

文献索引：Tomasi, Sophie; Renault, Jacques; Martin, Benedicte; Duhieu, Stephane; Cerec, Virginie; Le Roch, Myriam; Uriac, Philippe; Delcros, Jean-Guy Journal of Medicinal Chemistry, 2010 , vol. 53, # 21 p. 7647 - 7663

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被引用次数: 16

摘要

The polyamine transport system (PTS) whose activity is up-regulated in cancer cells is an attractive target for drug design. Two heterocyclic (azepine and benzazepine) systems were conjugated to various polyamine moieties through an amidine bound to afford 18 compounds which were evaluated for their affinity for the PTS and their ability to use the PTS for cell delivery. Structure− activity relationship studies and lead optimization afforded two ...