SYNTHESIS AND BIOLOGICAL PROPERTIES OF HYDROXYLAMINOPURINES AND RELATED DERIVATIVES

Syntheses are described for the preparation of substituted hydroxylaminopurines, the related methoxyamino, methylhydroxylamino, methylhydrazino, and methylmercapto derivatives, and some ribonucleosides thereof. These compounds were tested against L1210 mouse leukemia. Two compounds, 6-methoxyaminopurine and 2-hydroxylamino-6-methylmercaptopurine, were active against the parent L1210 line but not against a sub line resistant to 6-mercaptopurine, suggesting that they may be converted to active nucleotides by a mechanism similar to that of 6-mercaptopurine. © 1968, American Chemical Society. All rights reserved.