Cytotoxic dimeric epipolythiodiketopiperazines from the ascomycetous fungus Preussia typharum.
J Nat Prod
; 77(6): 1459-66, 2014 Jun 27.
Article
em En
| MEDLINE
| ID: mdl-24893224
ABSTRACT
Two new dimeric epipolythiodiketopiperazines, preussiadins A (1) and B (2), together with two known diastereomers, leptosins C (6) and A (7), were obtained from the mycelia of a Preussia typharum isolate. The structures of the new compounds were established by spectroscopic methods, and the absolute configurations of 1 and 2 were assigned by chemical transformations and comparisons of quantum chemical ECD and VCD calculations to experimental data. Compound 1 exhibited potent cytotoxic activity in the NCI-60 cell line panel with an average LC50 value of 251 nM. Further studies demonstrated that 1 circumvents P-glycoprotein-mediated drug resistance, yet had no significant antitumor activity in a xenograft UACC-62 melanoma model.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Ascomicetos
/
Antineoplásicos
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article