Sesquiterpenes with inhibitory activity against CDC25 phosphatases from the soft coral Pseudopterogorgia rigida

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• 作者：Panagiota Georgantea^a ; Efstathia Ioannou^a ; Emilie Evain-Bana^b ; Denyse Bagrel^b ; Nadine Martinet^c ; Constantinos Vagias^a ; ^&dagger ; ; Vassilios Roussis^a ; ^{roussis@pharm.uoa.gr" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Pseudopterogorgia rigida ; Bisabolane ; Cadinane ; Eleutherane ; CDC25 phosphatases inhibitory activity
• 刊名：Tetrahedron
• 出版年：2016
• 出版时间：9 June 2016
• 年：2016
• 卷：72
• 期：23
• 页码：3262-3269
• 全文大小：450 K

文摘

Twenty one sesquiterpenes were isolated from the organic extract of the Caribbean gorgonian Pseudopterogogia rigida. Among them, seven bisabolanes (boldFont">1, boldFont">2, boldFont">9–boldFont">11, boldFont">13 and boldFont">14), six cadinanes (boldFont">15–boldFont">20) and one sesquiterpene featuring a new tricyclic carbon skeleton (boldFont">21) are new natural products, while two (boldFont">6 and boldFont">7) are reported for the first time from a natural source. The structures of the new compounds were established by detailed analyses of their NMR and MS data. The isolated metabolites were evaluated for their inhibitory activity against CDC25 phosphatases, which represent possible targets related to cancer therapy. Compounds boldFont">4 and boldFont">18 were the most active with IC₅₀ values of 1.88 and 3.44 μM, respectively, against the CDC25A isoform.