Secrist J A, Shortnacy A T, Montgomery J A
J Med Chem. 1985 Nov;28(11):1740-2. doi: 10.1021/jm00149a033.
Syntheses of 2-fluoroformycin [7-amino-5-fluoro-3-(beta-D-ribofuranosyl)pyrazolo[4,3-d]pyrimidine] (2b) and 2-aminoformycin [5,7-diamino-3-(beta-D-ribofuranosyl)pyrazolo[4,3-d]pyrimidine] (2c) are described. Cytotoxicity data are given for 2b and 2c alone as well as with added pentostatin. Kinetic parameters for adenosine deaminase are also provided. 2-Fluoroformycin, although a much poorer substrate for adenosine deaminase than formycin A, is not nearly as cytotoxic to cells in culture.
描述了2-氟杀稻瘟菌素7-氨基-5-氟-3-(β-D-呋喃核糖基)吡唑并[4,3-d]嘧啶和2-氨基杀稻瘟菌素5,7-二氨基-3-(β-D-呋喃核糖基)吡唑并[4,3-d]嘧啶的合成。给出了2b和2c单独以及添加喷司他丁后的细胞毒性数据。还提供了腺苷脱氨酶的动力学参数。2-氟杀稻瘟菌素虽然作为腺苷脱氨酶的底物比杀稻瘟菌素A差得多，但对培养细胞的细胞毒性远没有那么大。
