Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 47, Issue -, Pages 424-431Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.11.011
Keywords
Diphyllin; Topo II inhibitors; Synthesis; Anticancer; Structure-activity relationship
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Recently, a novel glycosylated diphyllin derivative 11 which exhibiting potent anticancer activity by targeting topoisomerase II alpha was reported by our group. In order to provide more molecules for structure-activity relationship (SAR) studies, 12 new glycosylated diphyllin analogs have been designed, synthesized, and evaluated for their biological activities. The SAR analysis revealed that (i) the sugar moiety on the diphyllin is essential for the anticancer activity; (ii) equatorial C4 '-OH on the sugar is superior to the axial one, and (iii) a proper cyclic lipophilic group at the C4' and C6' of sugar might enhance the anticancer activity. (C) 2011 Elsevier Masson SAS. All rights reserved.
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