Synthesis and In-Vitro Antitumor Activity of Selected 7-Fluoro-6-(4-methyl- 1-piperazinyl)-2-(thiosubstituted)-4(3H)-quinazolinones

A new series of 7-fluoro-6-(4-methyl-1-piperazinyl)-2-(thiosubstituted)- 4(3H)-quinazolinones was synthesized as potential antitumor agents by multi-step synthesis starting with the commercially available 3-chloro-4-fluoroaniline. The most promising candidate, 7-fluoro-6-(4-methyl-1-thyl-1-piperazinyl)-2- thioethyl-4(3H)-quinazolinone (5a), was screened in 60 human cancer cells by NCI.