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Highly cytotoxic benzo[c]pyrido[2,3,4-kl]acridines
Sarah Chackal1, Michael Facompré, Raymond Houssin
1Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, Université de Lille 2, BP 83, 59006 Lille, France.
Bioorganic & Medicinal Chemistry Letters
|March 6, 2003
Abstract:
Several benzo[c]pyrido[2,3,4-kl]acridines bearing different substituents on the A and E rings were synthesized and evaluated for their capacity to bind to DNA and to inhibit DNA topoisomerases. Potent cytotoxic compounds were discovered but no strict correlation with their DNA binding affinity and effects on topoisomerases were observed. DNA is one but not the unique target of these compounds.