Synthesis, DNA binding and antitrypanosomal activity of benzimidazole analogues of DAPI

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Exploration of DAPI analogues: Synthesis, antitrypanosomal activity, DNA binding and fluorescence properties

The DAPI structure has been modified by replacing the phenyl group with substituted phenyl or heteroaryl rings. Twelve amidines were synthesized and their DNA binding, fluorescence properties, in vitro and in vivo activities were evaluated. These compounds are shown to bind in the DNA minor groove with high affinity, and exhibit superior in vitro antitrypanosomal activity to that of DAPI. Six n...

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ژورنال

عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters

سال: 2016

ISSN: 0960-894X

DOI: 10.1016/j.bmcl.2016.11.006