Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines

AA Farahat, A Kumar, M Say, AEDM Barghash…

文献索引：Farahat, Abdelbasset A.; Kumar, Arvind; Say, Martial; Barghash, Alaa El-Din M.; Goda, Fatma E.; Eisa, Hassan M.; Wenzler, Tanja; Brun, Reto; Liu, Yang; Mickelson, Leah; Wilson, W. David; Boykin, David W. Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 2 p. 557 - 566

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被引用次数: 15

摘要

A novel series of extended DAPI analogues were prepared by insertion of either a carbon– carbon triple bond (16a–d) or a phenyl group (21a, b and 24) at position-2. The new amidines were evaluated in vitro against both Trypanosoma brucei rhodesiense (T. br) and Plasmodium falciparum (P. f.). Five compounds (16a, 16b, 16d, 21a, 21b) exhibited IC50 values against T. br of 9nM or less which is two to nine folds more effective than DAPI. The ...