BISANTHRAPYRAZOLES AS ANTI-CANCER AGENTS

Disclosed are novel bisanthrapyrazoles that likely act as bisintercalators and topoisomerase Ila inhibitors. These compounds show potent inhibition of cancer cell growth, and certain bisanthrapyrazoles bind to DNA more tightly than doxorubicin, a known intercalating anti-cancer drug. Molecular model...

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Bibliographic Details
Main Authors GUZIEC, FRANK, HASINOFF, BRIAN, B, GUZIEC, LYNN, J, LIANG, HONG
Format Patent
LanguageEnglish
French
Published 08.01.2009
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Summary:Disclosed are novel bisanthrapyrazoles that likely act as bisintercalators and topoisomerase Ila inhibitors. These compounds show potent inhibition of cancer cell growth, and certain bisanthrapyrazoles bind to DNA more tightly than doxorubicin, a known intercalating anti-cancer drug. Molecular modeling techniques are also disclosed that allow one to predict the DNA binding strength of various intercalators. L'invention porte sur de nouveaux bisanthrapyrazoles qui agissent vraisemblablement comme bisintercalateurs et inhibiteurs de la topoisomérase Ila. Ces composés manifestent une inhibition puissante de la croissance des cellules cancéreuses, et certains bisanthrapyrazoles se lient à l'ADN plus étroitement que la doxorubicine, un médicament anticancer d'intercalation connu. L'invention porte également sur des techniques de modélisation moléculaire qui permettent de prédire la force de liaison à l'ADN de divers intercalateurs.
Bibliography:Application Number: WO2008IB02784