In vivo Antitumor Activity of Novel 3, 4 di-Substituted Quinazoline Derivatives: A Novel Approach

Abstract

This chapter discussed about in vivo antitumor activity of novel 3, 4 di-substituted quinazoline derivatives. Quinazolines were surveyed as biologically relevant moieties against different cancer cell lines. Series of 7-chloro-3-[substituted (amino/phenyl amino)]-2-phenyl quinazolin-4 (3H)-one/thione derivatives and 1-(7-chloro-4-oxo/-2-phenylquinazoline-3 (4H-yl)) substituted urea derivatives were synthesized and characterised by infrared (IR), H¹ nuclear magnetic resonance (NMR) and mass spectra (m/z) and elemental analysis. In Swiss albino mice exhibiting Ehrilich ascites carcinoma (EAC), the in-vivo anticancer activity was examined using a number of measures, including body weight analysis, mean survival time, and % increase in life span approaches.  Six compounds (IIh, IIi, IIj, IIIh, IIIi, IIIj)) have shown significant antitumor activity.

The research-derived quinazoline derivatives show that the amino group in the third position and the urea/thiourea group in the phenyl hydrazine ring in the third position of the quinzoline skeleton are crucial for anticancer action.  Compounds IIh, IIi, IIj, IIIh, IIIi and IIIj were found to be biologically active which may be useful as potential resource for the discovery of anti-tumor compound having common quinazoline pharmacophore with lesser toxic effects.