A comparative study of the anticancer activity of some S-substituted derivatives of 6-mercaptopurine and their ribonucleosides

JA Montgomery, TP Johnston, A Gallagher… - Journal of Medicinal …, 1960 - ACS Publications
JA Montgomery, TP Johnston, A Gallagher, CR Stringfellow, FM Schabel Jr
Journal of Medicinal Chemistry, 1960ACS Publications
Because of the established anticancer activity of 6-mercaptopurine1 [purine-6 (lH)-thione],
we prepared the ribonucleoside of this purine some time ago in these laboratories. 2 A
careful com-parative evaluation of the activity of this purine and itsribo-nucleoside against
Carcinoma 755, a tumour unusually sensitive to purine antagonists, in BDF 1 mice showed
the ribonucleoside to have a greater therapeutic index in this testsystem. 3 This initial result
led us to synthesize and test a number of ribonucleo-sides of¿-substituted derivatives of 6 …
Because of the established anticancer activity of 6-mercaptopurine1 [purine-6 (lH)-thione], we prepared the ribonucleoside of this purine some time ago in these laboratories. 2 A careful com-parative evaluation of the activity of this purine and itsribo-nucleoside against Carcinoma 755, a tumour unusually sensitive to purine antagonists, in BDF 1 mice showed the ribonucleoside to have a greater therapeutic index in this testsystem. 3 This initial result led us to synthesize and test a number of ribonucleo-sides of¿-substituted derivatives of 6-mercaptopurine. The¿-substituted 6-mercaptopurine derivatives themselves had been synthesized previously4 and found to have activity against Carcinoma 755.3
ACS Publications