Syntheses of 1-[(2-hydroxyethoxy)methyl]- and 1-[(1,3-dihydroxy-2-propoxy)methyl]- derivatives of 5-substituted-2,4-difluorobenzene: unnatural acyclo thymidine mimics for evaluation as anticancer and antiviral agents.
Nucleosides Nucleotides Nucleic Acids
; 19(9): 1397-411, 2000 Sep.
Article
en En
| MEDLINE
| ID: mdl-11092311
A group of 1-[(2-hydroxyethoxy)methyl]- (12) and 1-[(1,3-dihydroxy-2-propoxy)methyl]- (13) derivatives of 2,4-difluorobenzene possessing a variety of C-5 substituents (R = Me, H, I, NO2) were designed with the expectation that they may serve as acyclic 5-substituted-2'-deoxyuridine (thymidine) mimics. Compounds 12 and 13 (R = Me, H, I) were inactive as anticancer agents (CC50 = 10(-3) to 10(-4) M range), whereas the 5-nitro compounds (12d, 13d) exhibited weak-to-moderate cytotoxicity (CC50 = 10(-5) to 10(-6) M range) against a variety of cancer cell lines. All compounds prepared (12a-d, 13a-d) were inactive as antiviral agents in a broad-spectrum antiviral screen that also included the human immunodeficiency virus (HIV-1 and HIV-2) and herpes simplex virus (HSV-1 and HSV-2).
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Antivirales
/
Timidina
/
Derivados del Benceno
/
Antineoplásicos
/
Nucleósidos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Nucleosides Nucleotides Nucleic Acids
Asunto de la revista:
BIOQUIMICA
Año:
2000
Tipo del documento:
Article
País de afiliación:
Canadá
Pais de publicación:
Estados Unidos