Synthesis and in vitro cytotoxicity of 1,2,3,4-tetrahydroisoquinoline derivatives.
Eur J Med Chem
; 41(2): 241-52, 2006 Feb.
Article
en En
| MEDLINE
| ID: mdl-16412536
ABSTRACT
Several 1-alkyl-1,2,3,4-tetrahydroisoquinoline (TIQ) derivatives, which may play a role in Parkinson's disease, have been synthesized via Pummerer-type cyclization of the sulfonium ion formed in situ from N-formyl sulfoxide. Using an in vitro trypan blue exclusion assay, high concentrations of TIQ derivatives possessing bulky alkyl group substituents such as 1-cyclobutyl-, 1-cyclohexyl-, 1-phenyl- or 1-benzyl- at the C-1 position were found to significantly affect the viability of PC12 cells. Moreover, TIQ derivatives that moderately or strongly induced apoptosis (e.g., 1-phenyl-TIQ and 1-cyclohexyl-TIQ, respectively) paralleled the results obtained using the trypan blue exclusion assay. These results suggest that the size and electron-donating properties of functional groups may affect the cytotoxicity of TIQ derivatives.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Enfermedad de Parkinson
/
Encéfalo
/
Apoptosis
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Tetrahidroisoquinolinas
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Neurotoxinas
Límite:
Animals
Idioma:
En
Revista:
Eur J Med Chem
Año:
2006
Tipo del documento:
Article
País de afiliación:
Japón