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Gefitinib Synthetic Derivative Of Nepal

Posted on:2015-02-28Degree:MasterType:Thesis
Country:ChinaCandidate:Y X CuiFull Text:PDF
GTID:2261330431456531Subject:Organic Chemistry
Abstract/Summary:PDF Full Text Request
Quinazoline compounds and their derivatives have a variety of biological activity.Studies have shown that quinazoline compounds containing basic skeleton haveantibacterial, anti-inflammatory, anti-tuberculosis, anti-diabetic, anti-HIV andanti-tumor biological activity. In recent years, quinazoline compounds are hot topics inanticancer drug research, which have shown significant effect in the restraint of EGFR,RARP, MPS2, JAK2, CHK-2and Pin1etc. So far,22kinds of imatinib anticancer drugshave been successfully put into the market and have an outstanding curative effect, mostof which are quinazoline compounds, Imatinib, Gefitinib, Erlotinib and Lapatinib forexample. Thus the popular in studying quinazolines antineoplastic continusly increased.In this study, the backgroud of the application of quinazoline compounds inanticancer drugs are introduced, and after doing research in relevant literature, a designto modify the new quinazoline derivatives by changing the side chain6-and4-substituents, MTT assay is introduced to study its biological activity finally.In this study, tthese compounds we synthesized are testd on the cancer retraint ofMCF-7(human breast cancer cells) HEPG2(human hepatoma cells) A549(human lungcancer cells). The results show that the compounds we synthesized work well in restrainthe cancel cells. Compounds numbered CX-5, CX-12, CX-13even show a much highereffect than the original gefitinib drug, Compounds numbered CX-4, CX-6, CX-7CX-8,and CX-14show a comparable effect compared with gefitinib, which is a possiblecandidate for antineoplastic agents.
Keywords/Search Tags:Quinazoline, Key intermediates, Biological activity
PDF Full Text Request
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