2-Fluoroformycin and 2-aminoformycin. Synthesis and biological activity.
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.
D000241:Adenosine / Q000378:metabolism; D000243:Adenosine Deaminase / Q000378:metabolism; D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000627:therapeutic use*; D005573:Formycins / Q000138:chemical synthesis / Q000378:metabolism / Q000627:therapeutic use*; D007700:Kinetics; D007939:Leukemia L1210 / Q000188:drug therapy* / Q000378:metabolism; D009711:Nucleotides / Q000378:metabolism; D010710:Phosphates / Q000378:metabolism; D013379:Substrate Specificity
D000903:Antibiotics, Antineoplastic; D005573:Formycins; D009711:Nucleotides; D010710:Phosphates; C034550:formycin; C047242:2-aminoformycin; C047241:2-fluoroformycin; D000243:Adenosine Deaminase; D000241:Adenosine