SYNTHESIS OF NEW FLUORESCENT NUCLEOSIDES, 3-β-D-RIBOFURANOSYLPYRAZOLO [3, 2-i__-] PURINE DERIVATIVES AND THEIR CYTOTOXIC ACTIVITIES

Abstract

The novel nucleosides 3-β-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-β-D-ribofuranosyl [3, 2-i__-]purine-9-carboxyamide 1 by dromodeamidation (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 cytotoxity.