Synthesis of Quinazolinone Derivatives with Nitrogen Mustard as Possible Anticancer Agents

Abstract

A few series of 1-sustituted phenyl 2-[(bis-(2-chloroethyl)amino]- methyl-7-nitro-4(1H)-quinazolinone have been synthesized by chlorination of 1-sustituted phenyl 2-[(bis-(2-hydroxyethyl)amino]methyl- 7-nitro-4(1H)-quinazolinone with phosphorous oxychloride and phosphorous penta chloride. All the 7 compounds were incorporated with nitrogen mustard moiety. The synthesized compounds were screened for their anticancerous activity by short term in vitro antitumor activity and in vivo anticancer activity by body weight analysis, Mean survival time and percentage increase in life span methods in Swiss albino mice bearing DLA 1 × 10⁶ cells/mL. The structures of the synthesized compounds was confirmed by spectral analysis. Investigation of anticancer activity was done by using Daltons Lymphoma Ascites (DLA) cell line.