The structure-based design, synthesis, and biological evaluation of DNA-binding amide linked bisintercalating bisanthrapyrazole anticancer compounds

…, LJ Guziec, FS Guziec, K Marshall, JC Yalowich

文献索引：Hasinoff, Brian B.; Zhang, Rui; Wu, Xing; Guziec, Lynn J.; Guziec Jr., Frank S.; Marshall, Kyle; Yalowich, Jack C. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 13 p. 4575 - 4582

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被引用次数: 9

摘要

A series of amide-coupled bisanthrapyrazole derivatives of 7-chloro-2-[2-[(2-hydroxyethyl) methylamino] ethyl] anthra [1, 9-cd] pyrazol-6 (2H)-one (AP9) were designed using molecular modeling and docking and synthesized in order to develop an anticancer drug that formed a strongly binding bisintercalation complex with DNA. Concentration dependency for the increase in the DNA melting temperature was used to determine the ...