3,5-Bis(3′-indolyl)pyrazoles, analogues of marine alkaloid nortopsentin: Synthesis and antitumor properties

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• 作者：Patrizia Diana ; Anna Carbone ; Paola Barraja ; Annamaria Martorana ; Ornella Gia ; Lisa DallaVia ; Girolamo Cirrincione
• 关键词：Nortopsentins ; 3 ; 5-Bis(3′ ; -indolyl)pyrazoles ; Antitumor activity ; Topoisomerase II
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 November 2007
• 卷：17
• 期：22
• 页码：6134-6137
• 文件大小：177 K

摘要

A series of 10 bis-indolylpyrazoles of type 9, 10 were obtained by cyclization of diketones 8 using hydrazine monohydrate or methylhydrazine in refluxing acetic acid/THF. Derivatives 9a,c,d were selected, by the National Cancer Institute (NCI, Bethesda, USA), to be evaluated against the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity in the micromolar range. In particular, 9d, the most active compound was effective against all the tested cell lines with a GI₅₀ mean value of 3.23 μM; TGI and LC₅₀ values were 14.5 and 58.9 μM having positive response on 91%and 41%of the tested cell lines, respectively.