Design, synthesis, and biological evaluation of a novel series of bisintercalating DNA-binding piperazine-linked bisanthrapyrazole compounds as anticancer agents

R Zhang, X Wu, JC Yalowich, BB Hasinoff

Index: Zhang, Rui; Wu, Xing; Yalowich, Jack C.; Hasinoff, Brian B. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 23 p. 7023 - 7032

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Citation Number: 13

Abstract

A series of bisintercalating DNA binding bisanthrapyrazole compounds containing piperazine linkers were designed by molecular modeling and docking techniques. Because the anthrapyrazoles are not quinones they are unable to be reductively activated like doxorubicin and other anthracyclines and thus they should not be cardiotoxic. The concentration dependent increase in DNA melting temperature was used to determine the ...