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Reported in the literature from the point of view , 4 - (N- aryl ) amino substituted quinazoline compounds in inhibiting EGFR-TK has excellent performance , which shows higher antitumor activity , the representative compound is PD 153,035 . In this thesis, PD 153035 is the lead compound to 2,3,4 - trimethoxy benzoic acid as the starting material , after nitration , esterification with methanol , iron reduction , methanol and formamide loop sodium , phosphorus oxychloride chlorine and aromatic amines of 4 - bit amination , six -step reaction , designed and synthesized 23 5,6,7 - trimethoxy -4 - (N- aryl ) amino- quinazoline compounds, 22 of new compounds , and through IR, NMR, elemental analysis were characterized . Using microwave irradiation method and the conventional method for all target compounds 5,6,7 - trimethoxy -4 - (N- aryl ) amino quinazoline was synthesized , and these two methods were compared, the results show that microwave method shortens the reaction time ( from 2 ~ 12h shortened to 30min), improved yield ( ~ 71.6% increase from 30.1 to 80.1 ~ 90.0% ) , and post-processing is simple ; while the traditional method is not only long reaction time , low yield , and easy to make a halogen -containing aromatic amines and between adjacent aromatic amine halide compound to form a quinazoline hydrochloride. Anticancer activity of the test compound that most of the target compound to inhibit human prostate cancer (PC3) and human breast cancer (Bcap-37) two kinds of the activity of cancer , wherein the compound I 3 , I 6 , I 7 , I 8 , I 9 , I 11 and I 16 on PC3 cells with good inhibitory activity in 10μmol / L drug concentration on PC3 cells inhibition rates were 31.7% , 32.6% , 58.0% , 38.9% , 39.7% , 49.6% , 34.6% ; compound I 16 in 10μmol / L drug concentration on Bcap-37 cell inhibition rate reached 60.7% , with higher inhibitory activity. Selected compounds cytotoxicity experiments and found that compound I 1 , I 3 on PC3 cells toxicity.
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