Abstract: In this paper,Jones oxidation of the diol-type saponins of Panax notoginseng afforded compound 1.Its 3-carbonyl group was converted to amino group by reductive amination to give compound 2,and then compound 2 was reacted with sulfonyl chloride reagent to give compounds 3-12.The syntheses of the 11 derivatives have not been reported.Their structures were identified by ¹H-NMR, ¹³C-NMR and MS.Thier in vitro anti-tumor activities were evaluated against HL-60,SMMC-7721,A-549,MCF-7,SW480 cancer cells by MTS assay.The results showed that compound 9 had some anti-tumor activity and was worthy of further study.

Key words: panaxadiol type saponin of Panax notoginseng, sapogenins, sulfonamide, anti-tumor activity