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Bioorg Med Chem Lett. 2004 Jul 16;14(14):3659-63.

Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.

Author information

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

Abstract

Indenoisoquinolines and dihydroindenoisoquinolines have been synthesized possessing a nitro-substituted isoquinoline ring in an effort to explore the effects of electron-withdrawing substituents on biological activity. The in vitro anticancer activities of these molecules have been tested in the National Cancer Institute's screen of 55 cell lines. The compounds have also been tested for topoisomerase I (top1) inhibition. The results indicate that these substances are a potent class of top1 inhibitors with sub-micromolar cytotoxicity mean graph midpoints (MGM) and top1 inhibition equal to camptothecin.

PMID:
15203138
DOI:
10.1016/j.bmcl.2004.05.022
[Indexed for MEDLINE]

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