RESUMEN
A series of novel 2',3'-dideoxy-2',3'-diethanethioribonucleosides and those modified with a triazole ring were prepared in excellent yields and their antitumor activity was evaluated. Nucleosides with a triazole ring, 16a-16c, showed significantly improved activity towards a broad range of tumor cell lines.
Asunto(s)
Antineoplásicos/síntesis química , Tionucleósidos/síntesis química , Triazoles/química , Antineoplásicos/química , Antineoplásicos/farmacología , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Células HeLa , Células Hep G2 , Humanos , Espectroscopía de Resonancia Magnética , Tionucleósidos/química , Tionucleósidos/farmacologíaRESUMEN
A new type of NADH model compound with good reactivity and enantioselectivity has been synthesized in good yields by an efficient and convenient synthetic method. The structures of these model compounds were confirmed by 1H and 13C-NMR and MS.
Asunto(s)
Formiatos/síntesis química , Ácidos Mandélicos/química , NAD/química , Formiatos/química , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , EstereoisomerismoRESUMEN
A series of novel 2',3'-diethanethio-2',3',5'-trideoxy-5'-triazoloribonucleosides was synthesized in excellent yields and their antitumor activity was evaluated. These nucleoside analogues with aromatic substituted triazole rings showed significantly improved activity towards a broad range of tumor cell lines and those without arene substitutes were inactive.