Design, synthesis and biological evaluation of some novel substituted quinazolines as antitumor agents

• A novel series of 6-chloro-2-p-tolylquinazolinone were designed and synthesized.
• The synthesized compounds were evaluated for their in-vitro antitumor activity.
• Compound 16 possessed broad-spectrum antitumor activities.
• Compound 16 has 1.5-fold potency compared to 5-FU.

A novel series of 6-chloro-2-p-tolylquinazolinone and substituted-(4-methylbenzamido)benzamide (1–20) were designed, synthesized and evaluated for their in-vitro antitumor activity. Compounds 3, 14 and 16 possessed remarkable broad-spectrum antitumor activity. Compound 16 was found to be a particularly active growth inhibitor of the renal cancer (GI50 = 4.07 μM), CNS cancer (GI50 = 7.41 μM), ovarian cancer (GI50 = 7.41 μM) and non-small cell lung cancer (GI50 = 7.94 μM). Compound 16 ranks as nearly 1.5-fold more potent (mean GI50 = 15.8 μM) compared to 5-FU (mean GI50 = 22.6 μM).

Compound 16 possessed broad-spectrum antitumor activities with 1.5-fold potency (mean GI50 = 15.8 μM), compared to 5-FU (mean GI50 = 22.6 μM).Figure optionsDownload as PowerPoint slide