Syntheses and structure-activity relationship studies of N-substituted-β-D-glucosaminides as selective cytotoxic agents.
Twenty-four diosgenyl saponins bearing cinnamoyl, carbamido and thiosemicarbazone groups were synthesized concisely. The cytotoxicities of the synthetic compounds on six human caner cell lines were evaluated employing MTT method. Structure-activity relationship could be observed, and two of the synthesized compounds (5c and 5f) exhibited selective inhibition on HeLa and MCF-7 cells, while three of them (5d, 5f and 5h) showed strong inhibition against HT1080.
Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Bo
B
Wang
Yang
Y
Liu
Yanshi
Y
Wang
Xin
X
Liu
Mao-Sheng
MS
Cheng
D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D061986:MCF-7 Cells; D012503:Saponins / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D013329:Structure-Activity Relationship; D013882:Thiosemicarbazones / Q000737:chemistry; D014508:Urea / Q000737:chemistry
D012503:Saponins; D013882:Thiosemicarbazones; D014508:Urea