Purdue Research Foundation

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

National Institutes of Health (nih)

Daniel Edward Beck

Mark Stanley Cushman

Yves Pommier

Andrew E Morrell

Keli K Agama

Smitha Antony

Muthukaman Nagarajan

The invention described herein pertains to four series of aza-A-ring indenoisoquinolines, which are inhibitors of topoisomerase IB (Top1), and the processes for preparing said aza-A-ring indenoisoquinolines. Also described are methods for treating cancer in mammals using the described aza-A-ring indenoisoquinoline compounds or pharmaceutical formulations thereof.

Aza-A-ring indenoisoquinoline topoisomerase I poisons

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 indenoisoquinoline compounds as described herein, wherein R, R, W, X and Y are defined herein, pharmaceutical compositions and formulations comprising the indenoisoquinoline compounds, their synthesis, and methods for their use in the treatment and/or prevention of cancer.

Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors

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Lafayette, IN, United States of America

Daniel Edward Beck