Design, Synthesis, and Biological Evaluation of Novel Dual Inhibitors of Secretory Phospholipase A2 and Sphingomyelin Synthase

Autor:	Peng Men, Gong Haojun, Deyong Ye, Xing Gao, Lu Zhou
Rok vydání:	2013
Předmět:	Indole test biology Chemistry Cyanide Cell In vitro toxicology General Chemistry Secretory Phospholipase A2 chemistry.chemical_compound medicine.anatomical_structure Biochemistry Design synthesis Sphingomyelin synthase medicine biology.protein Biological evaluation
Zdroj:	Chinese Journal of Chemistry.
ISSN:	1001-604X
Popis:	A novel series of eight SMS and sPLA2 dual inhibitors containing indole and α-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 5e ideal for liver homogenate and SMS2 high expression cell homogenate, respectively.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::734b462e654ec7c43ca2328548e49437 https://doi.org/10.1002/cjoc.201300079 Zobrazit plný text záznamu Plný text