Antineoplastic agents. 1. Synthesis and antineoplastic activities of chloroethyl- and methylnitrosourea analogs of thymidine

Abstract

A new class of chloroethyl- and methylnitrosourea analogs of thymidine was synthesized from the corresponding amino nucleosides. The 3''-chloroethyl and 3''-methyl derivatives inhibited L1210 [mouse leukemia] cell growth in culture (ED50 = 1.5 and 1.0 .mu.M, respectively) more effectively than 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) (ED50 = 4 .mu.M) and the 5''-nitrosourea analogues. Neither the alkylating nor carbamoylating activities of these compounds correlated with their biological activity.