Synthesis, metabolism and in vitro cytotoxicity studies on novel lavendamycin antitumor agents.
Bioorg Med Chem
; 18(5): 1899-909, 2010 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-20149966
ABSTRACT
A series of lavendamycin analogues with two, three or four substituents at the C-6, C-7 N, C-2', C-3' and C-11' positions were synthesized via short and efficient methods and evaluated as potential NAD(P)Hquinone oxidoreductase (NQO1)-directed antitumor agents. The compounds were prepared through Pictet-Spengler condensation of the desired 2-formylquinoline-5,8-diones with the required tryptophans followed by further needed transformations. Metabolism and toxicity studies demonstrated that the best substrates for NQO1 were also the most selectively toxic to NQO1-rich tumor cells compared to NQO1-deficient tumor cells.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Estreptonigrina
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2010
Tipo de documento:
Article
País de afiliação:
Estados Unidos