Synthesis and cytotoxic evaluation of eremophilane sesquiterpene 07H239-A derivatives.
Chem Pharm Bull (Tokyo)
; 59(9): 1186-9, 2011.
Article
em En
| MEDLINE
| ID: mdl-21881269
ABSTRACT
Nine new derivatives (6-14) of the eremophilane sesquiterpene 07H239-A (5) were designed and semisynthesized with two types of R-groups by amidation. Most of them were active against five human tumor cell lines, and compounds 6-10 were more potent than the natural product 5. In particular, compounds 6 and 9 exhibited the strongest cytotoxic activity against MDA-MB-435 with IC50 values of 0.91 and 0.96 µM, respectively. Preliminary structure-activity relationships (SARs) analysis indicated that the 14-carboxyl in 5 was an ideal target for chemical modification, and the side chain of 5 might play a necessary role in facilitating their cytotoxic potencies.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Sesquiterpenos
/
Naftalenos
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Revista:
Chem Pharm Bull (Tokyo)
Ano de publicação:
2011
Tipo de documento:
Article