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Modified jatrophane diterpenes as modulators of multidrug resistance from Euphorbia dendroides L.

作者信息

Corea Gabriella, Fattorusso Ernesto, Lanzotti Virginia, Taglialatela-Scafati Orazio, Appendino Giovanni, Ballero Mauro, Simon Pierre Noël, Dumontet Charles, Di Pietro Attilio

机构信息

Dipartimento di Chimica delle Sostanze Naturali, Università di Napoli 'Federico II', Via D. Montesano 49, I-80131, Napoli, Italy.

出版信息

Bioorg Med Chem. 2003 Nov 17;11(23):5221-7. doi: 10.1016/j.bmc.2003.08.013.

DOI:10.1016/j.bmc.2003.08.013
PMID:14604686
Abstract

The new diterpenoids terracinolides J-L (1-3), 13alpha-OH terracinolide F (8), abeodendroidin F (11) and epiabeodendroidin F (12) have been identified from Euphorbia dendroides L. The new compounds and six co-occurring known terracinolides were tested as inhibitors of the drug-efflux activity of P-glycoprotein from cancer cells. The results were used to extend the structure-activity relationships established for this class of compounds highlighting the relevance of substitution at positions 2, 3, 6, and 15 and disclosing a remarkable tolerance toward connectivity changes in the terpenoid core.

摘要

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