Potential inhibitors of nucleotide biosynthesis. 2. Halomethyl ketone derivatives of pyrimidine nucleosides

Abstract
Several halomethyl ketone derivatives of pyrimidine nucleosides were prepared for evaluation as cytotoxic agents. The first series are 1-(8-halo-2,5,6,8-tetradeoxy-.beta.-D-erythro-oct-7-ulofuranosyl)thymines (7-9), whereas the 2nd type are halo derivatives of acetophenone (12-14 and 16). These compounds are cytotoxic, and one (13) [N-[4-(bromoacetyl)phenyl]-1,2-dideoxy-1-[3,4-dihydro-5-methyl-2,4-dioxo-1(2H)-pyrimidinyl]-.beta.-D-erythro-1-pentofuranuroamide] showed activity against the P388 leukemia in vivo.