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Bioorg Med Chem Lett. 2005 Jun 2;15(11):2795-8.

Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.

Author information

1
Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, IN 47907, USA.

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.

PMID:
15911256
DOI:
10.1016/j.bmcl.2005.03.101
[Indexed for MEDLINE]

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