A novel series of eight SMS and sPLA2 dual inhibitors containing indole and a-amino cyanide fragments of different length and substitution position was synthesized and evaluated by three different in vitro assays. Bio...A novel series of eight SMS and sPLA2 dual inhibitors containing indole and a-amino cyanide fragments of different length and substitution position was synthesized and evaluated by three different in vitro assays. Biological evaluation showed that all compounds provided inhibitory effects against SMS （about 50% inhibition at 100 μmol/L） and sPLA2 （14-32 μmol/L）. All the compounds had the SMS activity better than the positive control compound D609 in SMS2 homogenate, with compounds 5b and fie ideal for liver homogenate and SMS2 high expression cell homogenate, respectively.展开更多
基金The work was funded by the National Natural Science Foundation of China，Specialized Research Fund for the Doctoral Program of Higher Education，Chinese Ministry of Education,the open grant of the State Key Laboratory of Bio-organic and Natural Products Chemistry,CAS,and open grant of Institute of Bioscience,Fudan University
文摘A novel series of eight SMS and sPLA2 dual inhibitors containing indole and a-amino cyanide fragments of different length and substitution position was synthesized and evaluated by three different in vitro assays. Biological evaluation showed that all compounds provided inhibitory effects against SMS （about 50% inhibition at 100 μmol/L） and sPLA2 （14-32 μmol/L）. All the compounds had the SMS activity better than the positive control compound D609 in SMS2 homogenate, with compounds 5b and fie ideal for liver homogenate and SMS2 high expression cell homogenate, respectively.
