Structure-activity relationships in the acronycine and benzo[b]acronycine series: role of the pyran ring.
Eur J Med Chem
; 43(12): 2677-87, 2008 Dec.
Article
em En
| MEDLINE
| ID: mdl-18342404
ABSTRACT
In order to explore the structure-activity relationships in the acronycine series, simplified analogues of cis-1,2-diacetoxy-1,2-dihydroacronycine and cis-1,2-diacetoxy-1,2-dihydrobenzo[b]acronycine (S23906-1, under clinical trials) lacking the fused pyran ring, but possessing an acetoxymethyl leaving group at position 4 were prepared. These new analogues only displayed marginal antiproliferative activity compared to the parent compounds. The presence of the angularly fused dimethylpyran ring appears as an indispensable structural requirement to observe significant cytotoxic activity in this series.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Acronina
/
Antineoplásicos
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article