The syntheses and properties of tricyclic pyrrolo[2,3-d]pyrimidine analogues of S6-methylthioguanine and O6-methylguanine.
Org Biomol Chem
; 4(9): 1723-9, 2006 May 07.
Article
en En
| MEDLINE
| ID: mdl-16633564
ABSTRACT
The syntheses of novel tricyclic pyrrolo[2,3-d]pyrimidine analogues of S6-methylthioguanine are described. The crystal structures and pKa values of these and related O6-methylguanine analogues are reported. All compounds display higher pKa values than O6-methylguanine with the sulfur-containing analogues being the more basic and exhibiting higher stability in aqueous solution. In a standard substrate assay with the human repair protein O6-methylguanine-DNA methyltransferase (MGMT) only the oxygen-containing analogue displayed activity.
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Banco de datos:
MEDLINE
Asunto principal:
Pirimidinas
/
Pirroles
/
Tioguanina
/
Guanina
Límite:
Humans
Idioma:
En
Año:
2006
Tipo del documento:
Article