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

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• 作者：Abdelbasset A. Farahat^a ; ^b ; ^{afarahat@gsu.edu} ; Cheree Bennett-Vaughn^a ; Ekaterina M. Mineva^a ; Arvind Kumar^a ; Tanja Wenzler^c ; ^d ; Reto Brun^c ; ^d ; Yang Liu^a ; W. David Wilson^a ; David W. Boykin^a
• 关键词：Benzimidazole diamidines ; DAPI ; DNA minor groove binders ; Antitrypanosomal activity
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 December 2016
• 年：2016
• 卷：26
• 期：24
• 页码：5907-5910
• 全文大小：1244 K
• 卷排序：26

文摘

New analogues of the antitrypanosomal agent DAPI were made. ΔTm of some of the final amidines was superior than that of DAPI. Compounds 5b and 15a showed superior antitrypanosomal activity compared to the parent I.