Synthesis And Antitumor Activity Of Novel Quinazoline Derivatives Containing Acrylamide

In order to find efficient and low toxicity anti-tumor drugs, a series of novel quinazoline derivatives containing N-(3-aminophenyl)acrylamide were synthesized and their antiproliferative activities were evaluated against three human cancer cell lines (H1975, PC-3, MGC-803) by using methyl thiazolyl tetrazolium (MU) assay. The results showed that most compounds exhibited better antiproliferative activities against the four human tumor cell lines. Among them, N-(3-(2-((4-((4-chlorophenyl)amino)-7-methoxy- qiiinazolin-6-yeoxy)acetamido)phenypacrylamide (13j) showed the best antiproliferative activity against H1975 and MGC-803 cancer cell lines with IC50 values of (6.77 +/- 0.65) and (4.06 +/- 0.34) mu mol/L, respectively. Its activity was better than the positive control gefitinib. In a nutshell, this work provides clues to discover antitumor agent based on the quinazoline scaffold.