Modified jatrophane diterpenes as modulators of multidrug resistance from Euphorbia dendroides L.
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.
Corea
Gabriella
G
Dipartimento di Chimica delle Sostanze Naturali, Università di Napoli 'Federico II', Via D. Montesano 49, I-80131, Napoli, Italy.
Fattorusso
Ernesto
E
Lanzotti
Virginia
V
Taglialatela-Scafati
Orazio
O
Appendino
Giovanni
G
Ballero
Mauro
M
Simon
Pierre Noël
PN
Dumontet
Charles
C
Di Pietro
Attilio
A
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors; D045744:Cell Line, Tumor; D004224:Diterpenes / Q000494:pharmacology*; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D028481:Euphorbia / Q000737:chemistry*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D016339:Spectrometry, Mass, Fast Atom Bombardment
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D004224:Diterpenes