Dicationic DNA-targeted antiprotozoal agents: naphthalene replacement of benzimidazole

S Chackal-Catoen, Y Miao, WD Wilson…

文献索引：Chackal-Catoen, Sarah; Miao, Yi; Wilson, W. David; Wenzler, Tanja; Brun, Reto; Boykin, David W. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 22 p. 7434 - 7445

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被引用次数: 25

摘要

A series of naphthalene analogues of highly active benzimidazole diamidines were synthesized using sequential Stille and Suzuki coupling reactions for preparation of the bis- nitrile intermediates. All of the diamidines showed strong DNA affinities as judged by high ΔTm values with poly (dA–dT). The dicationic compounds were quite active in vitro versus Trypanosoma brucei rhodesiense (T. br) exhibiting IC50 values ranging from 4 to 98nM. ...