Journal
CHINESE JOURNAL OF CHEMISTRY
Volume 31, Issue 9, Pages 1164-1170Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cjoc.201300079
Keywords
atherosclerosis; secretory phospholipase A2 (sPLA2); sphingomyelin synthase (SMS); multi-target drug design; dual inhibitors
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Funding
- National Natural Science Foundation of China [30973641, 20902013]
- Specialized Research Fund for the Doctoral Program of Higher Education [20090071110054]
- Chinese Ministry of Education
- State Key Laboratory of Bio-organic and Natural Products Chemistry, CAS
- Institute of Bioscience, Fudan University
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A novel series of eight SMS and sPLA2 dual inhibitors containing indole and -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 mu mol/L) and sPLA2 (14-32 mu mol/L). All the compounds had the SMS activity better than the positive control compound D609 in SMS2 homogenate, with compounds 5b and 5e ideal for liver homogenate and SMS2 high expression cell homogenate, respectively.
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