Synthesis and Antitumor Activity of 2-Alkanesulfinyl (or Alkanesulfonyl)-7-methyl-5H-1, 3, 4-thiadiazolo[3, 2-a]pyrimidin-5-ones

Abstract

The repressing effect on the propagation of cultured Ehrlich ascites tumor cells by 1, 3, 4-thiadiazolo[3, 2-a]pyrimidine and s-triazolo[1, 5-a]pyrimidine derivatives was examined. Then the relationship between structure and activity as to a series of active compounds was discussed.
The results showed that substituent groups on the 2-position of 1, 3, 4-thiadiazolo[3, 2-a]pyrimidine took an important part to reveal the cytotoxic activity. Especially, the strong activity was found among the compounds which had electrophilic substituents such as alkylsulfoxide, alkylsulfone at the 2-position.