Synthesis and Anti-Proliferative Activity of Sulfanyltriazolylnaphthalenols and Sulfanyltriazolylnaphthalene-1,4-diones

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• 作者：Ibrahim Chaaban ; El Sayeda M. El Khawass ; Heba A. Abd El Razik ; Nehad S. El Salamouni ; Mariano Redondo-Horcajo ; Isabel Barasoain ; José ; Fernando Dí ; az ; Jari Yli-Kauhaluoma and Vâ ; nia M. Moreira
• 刊名：Archiv der Pharmazie
• 出版年：2016
• 出版时间：September 2016
• 年：2016
• 卷：349
• 期：9
• 页码：749-761
• 全文大小：840K
• ISSN：1521-4184

文摘

A series of new sulfanyltriazolylnaphthalenols (10a–f and 13a–f) and sulfanyltriazolylnaphthalene-1,4-diones (14a–f) were synthesized and evaluated against a panel of cancer cell lines. Among the tested compounds, 10b and 10d showed the best anti-proliferative activity with GI₅₀ values ranging from 2.72 to 10 and 3.13 to 13.1 µM, respectively, in several of the tumor cell lines tested. Compound 10d is highly selective toward leukemia cell lines and can be regarded as a good model for the development of new anti-leukemic agents.