RIBOFURANOSIDES OF CYTOSTATIC THYMINE DERIVATIVES OF 2-IMIDAZOLETHIONE

Ribofuranosides of cytostatic thymine derivatives of 2-imidazolethione. The growth of Ehrlich ascites carcinoma (fluid form) in mice is completely inhibited by thymine thioethers of 2-imidazolethione. In order to examine the possible iNvivo conversion of these derivatives of pyrimidine bases to nucleosides, two different methods have been evolved for the synthesis of β-Dribofurano-sides of thymine thioethers. These nucleosides exhibit less inhibitory activity than the corresponding bases and are cleaved by a crude enzyme preparation of Ehrlich ascites cells (uridinephosphorylase). On the other hand, the enzymatic synthesis of these nucleosides from the corresponding bases and ribose 1-phosphate failed. © 1969, IEEE. All rights reserved.