Abstract
Compounds 15, 16 and 19 possessed the most remarkable broad-spectrum antitumor activities, additionally; compound 15 almost sevenfold more active than the known drug 5-FU with GI50 values of 3.16 and 22.60μM, respectively.
A novel series of 2-(3-phenethyl-4(3H)quinazolin-2-ylthio)-N-substituted anilide and substituted phenyl 2-(3-phenethyl-4(3H) quinazolin-2-ylthio)acetate were designed, synthesized and evaluated for their in-vitro antitumor activity. Compound 15 possessed remarkable broad-spectrum antitumor activity which almost sevenfold more active than the known drug 5-FU with GI50 values of 3.16 and 22.60μM, respectively. Compound 15 exhibited remarkable growth inhibitory activity pattern against renal cancer (GI50=1.77μM), colon cancer (GI50=2.02μM), non-small cell lung cancer (GI50=2.04μM), breast cancer (GI50=2.77μM), ovarian cancer (GI50=2.55μM) and melanoma cancer (GI50=3.30μM). Docking study was performed for compound 15 into ATP binding site of EGFR-TK which showed similar binding mode to erlotinib.