[Synthesis, cytostatic activity and mechanism of action of N-glycosylhalomethylazoles. A new class of alkylating agents].
A model to produce a new type of alkylating agents having anti-cancer activity is described. They consist of a halomethyl-azol group of the benzyl type as alkylating center, and a sugar moiety as a carrier fragment. Alkylating nucleosides were produced as halomethyl-pyrazole, -imidazole, 1.2.3-triazole, and 1.2.4-triazole derivatives following the model, and tested upon Ehrlich ascites cancer and P-388 lymphocytic leukemia.
D000477:Alkylating Agents / Q000138:chemical synthesis / Q000627:therapeutic use*; D000818:Animals; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy*; D007093:Imidazoles / Q000138:chemical synthesis / Q000627:therapeutic use; D066298:In Vitro Techniques; D007941:Leukemia P388 / Q000188:drug therapy*; D007942:Leukemia, Experimental / Q000188:drug therapy*; D008545:Melanoma / Q000188:drug therapy*; D009005:Monosaccharides / Q000138:chemical synthesis / Q000627:therapeutic use*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000627:therapeutic use; D014230:Triazoles / Q000138:chemical synthesis / Q000627:therapeutic use
D000477:Alkylating Agents; D007093:Imidazoles; D009005:Monosaccharides; D011720:Pyrazoles; D014230:Triazoles
Sintesis, actividad citostática y mecanismo de acción de N-glicosil-halometil-azoles. Un nuevo tipo de agentes alquilantes.