| 3,3′-Disubstituted-2-oxindoles bearing a quaternary Stereogenic center1 are widely present in natural products and bioactive molecules.Isatin morita – baylis-hilleman carbonate of allyl alkylation reaction is a kind of very novel and effective method to build three quaternary carbon chiral center.This article will connect a good biological activity of 3,5-dimethyl 4 – nitro oxazole to 3-oxidation indoles framework through isatin morita-bay-hilleman carbonate of allyl alkylation reaction,and modify structure.With two active skeleton link,we hope that the new compound will express in the foundation of original structure more active targets and active mechanism,can be improved of activity of the original drug molecules,and could solve the problem of the original drug multi-drug resistance.we have screened conditions of the synthesis of target products including solvent and lewis base and used the conditions to get 15 compounds.Subject to further explore,the series compounds of 3,5-Dimethyl-4-nitroisoxazole splicing oxoindole alkaloid has been tested for K562,A549,PC-3.The antitumor activity experimenthas has got six(JDH002,JDH004,JDH006,JDH007,JDH008,JDH009)highly antitumor activity compounds like cisplatin.In order to get better active compounds,we selected JDH008 to increase its water solubleness and test the compound for K562.We selected JDH002 to reforme the structure of opening oxoindole ring and test the compound for PC-3.According to other literatures,different oxazole structure exist in a large number of antibacterial compounds.Therefore,subject has extended the compounds of ring opening of oxoindole indole and has got the 16 products to test antimicrobial activity. |
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