Synthesis of 5,6-dihydropyrrolo[2,1-a]isoquinolines featuring an intramolecular radical-oxidative cyclization of polysubstituted pyrroles, and evaluation of their cytotoxic activity.
Org Biomol Chem
; 8(19): 4374-82, 2010 Oct 07.
Article
em En
| MEDLINE
| ID: mdl-20672155
A three-step protocol for the synthesis of 1,2,3,8,9-pentasubstituted-5,6-dihydropyrrolo[2,1-a]isoquinolines is described, using van Leusen's polysubstituted pyrrole construction followed by intramolecular radical-oxidative cyclization of the isoquinoline system. The cytotoxic activities of the dihydropyrroloisoquinolines were tested on six tumor cell lines. Preliminary structure-activity studies revealed the importance of the identity of the aromatic substituent at the C-2 position, particularly a phenyl, m-(amino) phenyl or m-(cyclohexylmethylpiperazinamide) phenyl substituent, for cytotoxic activity.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirróis
/
Isoquinolinas
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article