Synthesis of new fluorescent nucleosides, 3-beta-D-ribofuranosylpyrazolo (3,2-i) purine derivatives and their cytotoxic activities.
The novel nucleosides 3-beta-D-ribofuranosylpyrazolo(3,2-i) purine (8) and their 9-substituted bromo, nitro and amino compounds (3, 6 and 11) have been prepared from a fully protected 3-beta-D-ribofuranosyl(3,2-i)purine-9-carboxyamide 1 by bromodeamidation (ipso bromination). Compounds 3, 8 and 11 exhibited antileukemic activity against mouse leukemia L5178Y cells in culture, while the 9-substituted nitro, ester and amide compounds (6, 12 and 13) showed no cytotoxicity.
Hamamichi
N
N
School of Pharmaceutical Science, Showa University, Tokyo, Japan.
Miyasaka
T
T
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D007940:Leukemia L5178 / Q000188:drug therapy*; D051379:Mice; D011684:Purine Nucleosides / Q000138:chemical synthesis* / Q000494:pharmacology; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D011684:Purine Nucleosides; D011720:Pyrazoles