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ID: ALA1145275

Journal: Bioorg Med Chem Lett

Title: Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.

Authors: Xiao X, Miao ZH, Antony S, Pommier Y, Cushman M.

Abstract: Dihydroindenoisoquinolines are analogs of cytotoxic indenoisoquinoline topoisomerase I (Top1) inhibitors, exhibiting potent cytotoxicity but weak inhibitory activity toward Top1. Through COMPARE analysis, cytotoxicity studies in Top1-deficient cells, chemical synthesis and biological evaluation of methylated dihydroindenoisoquinoline 5, we demonstrated that dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines in cancer cells.

CiteXplore: 15911256

DOI: 10.1016/j.bmcl.2005.03.101