Purdue Research Foundation

National Institutes of Health, a Component of the US Dept. of Health & Human Services

National Institutes of Health (nih)

Andrew E Morrell

Mark Stanley Cushman

Yves Pommier

Keli K Agama

Muthukaman Nagarajan

Smitha Antony

Daniel Edward Beck

Evgeny A Kiselev

Yves G Pommier

N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof.

N-substituted indenoisoquinolines and syntheses thereof

The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.

Azaindenoisoquinoline topoisomerase I inhibitors

Indenoisoquinolines and dihydroindenoisoquinolines are described. In particular, such compounds possessing one or more electron withdrawing substituents are described. The in vitro anticancer activities of these molecules tested in the National Cancer Institute's screen of 55 cell lines is described. The compounds tested for topoisomerase I (top1) inhibition is described.

Synthesis of indenoisoquinolines

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Andrew E Morrell