Sesquiterpenes with inhibitory activity against CDC25 phosphatases from the soft coral Pseudopterogorgia rigida. Issue 23 (9th June 2016)

• Record Type: Journal Article
• Authors: Georgantea, Panagiota; Ioannou, Efstathia; Evain-Bana, Emilie; Bagrel, Denyse; Martinet, Nadine; Vagias, Constantinos; Roussis, Vassilios
• Is Part Of: Tetrahedron. Volume 72:Issue 23(2016)
• Page Start: 3262
• Page End: 3269
• Publication Date: 2016-06-09
• Subjects: Pseudopterogorgia rigida -- Bisabolane -- Cadinane -- Eleutherane -- CDC25 phosphatases inhibitory activity; Chemistry, Organic -- Periodicals; 547.005
• DOI: 10.1016/j.tet.2016.04.059
• Languages: English
• ISSNs: 0040-4020

Abstract

Abstract: Twenty one sesquiterpenes were isolated from the organic extract of the Caribbean gorgonian Pseudopterogogia rigida . Among them, seven bisabolanes (1, 2, 9 –11, 13 and14 ), six cadinanes (15 –20 ) and one sesquiterpene featuring a new tricyclic carbon skeleton (21 ) are new natural products, while two (6 and7 ) 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. Compounds4 and18 were the most active with IC50 values of 1.88 and 3.44 μM, respectively, against the CDC25A isoform. Graphical abstract: