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We have developed a versatile method to synthesize novel cationic lipids: Firstly, we synthesized different generations of polyamidoamine dendrons with azide functional group;secondly, we prepared a series of hydrophobic molecules by modification of natural fatty acids with alkynyl group;At last, we conjugated the two parts through CuAAC catalyzed click chemistry.The synthesis method is simple, efficient and highly versatile.The obtained cationic lipids have good biocompatibility demonstrated by MTT assay.They can effectively form lipoplexes with plasmid DNA and transfect HEK293 cells with good activity, as estimated by agarose gel electrophoresis and green luciferase test.Besides, the aggregates formed by the cationic lipids displayed strong photoluminescence, broad absorption, and emission spectra.We observed the intracellular uptake efficiency of the cationic lipids by fluorescence microscopy and quantified by flow cytometry.The cationic lipids show promise as gene vehicles that can achieve delivery, transfection, and bioimaging at the same time.