Study On The Synthesis And Biological Activity Of New 1,2,3,4-tetrahydroquinoline Derivatives

It has attracted continuous interest to develop new drugs which have more effective and less side . Therefore, it is important to search many excellent leading compounds .The tetrahydroquinoline moiety is present in various natural products, and many tetrahydroquinoline derivatives exhibit a broad range of biological activities. Therefore, many new tetrahydroquinoline derivatives were synthesize and tested for antitumor activities, among which certain 2, 3, 4-trisubstituted tetrahydroquinoline deriva -tives were found to have fine antitumor activities. Thus we regarded one of these derivatives which have good activities as leading compounds to prepare aryl aimine-substituted furano or pyranoquinoline derivatives with Lewis acid which catalyzed aza-Diels -Alder reaction of N-arylimines with various dienophiles and test their antitumor activities .In this assay, we synthesized 22 compounds containing 10 target compounds . 8 of these target compounds are new compounds. Their chemical structures are confirmed by 'H-NMR, IR and MS spectrums. Their purity all exceed 97%. Preliminary tests to inhibit tumour cell of HL-60 in vitro show that 2of them have fine antitumor activities. This initially has testified our idea and set up the basis for further studying SAR of this kind of compounds.