L-alpha-amino Acid Ethyl Ester Derivatives, Structure And Biological Activity Determination

In order to search the introduction compounds for the novel anticancer drugs, four series of ethyl L-α-amino-acid ester derivatives:L-N-(2-thiophenesulfonyl)-α-amino-acid ethyl ester(Ⅰ), L-N-(β-pyridylformylaminothiono)-α-amino-acid ethyl ester (Ⅱ), L-N-[S-(+)-3-methyl-2- (4-chlorophenyl)butyrylaminothiono]-α-amino-acid ethyl ester (Ⅲ) and L-N-(2,4-dichloro- phenoxyacetaminothiono)-α- amino-acid ethyly ester (Ⅳ) were designed and synthesized. All of the target compounds are new compounds and their structures were confirmed by IR, 1H NMR, MS and elementary analysis. Their physical properties, spectrum properties, synthesis methods and reaction conditions were discussed as well. The structure formulas of the title compounds are as follows respectively:Further more, in order to investigate the relationship between the structure of compound and its property, the crystals of compounds (Ⅰa), (Ⅰe) andⅡd were successfully prepared and their structures were determined by single crystal X-Ray diffraction analysis. Some basic reseraches on their structures and activities were discussed. The preliminary biological activities tests of the target compounds were finished by using MTT assay. The preliminary results indicated that some target compounds of (Ⅰ)^Ⅳ have good inhibitory effect on the cell growth in vitro through affecting the metabolism of the tumor cells.By now, the activity tests of pesticide are processing in the Bayer Corporation.