論文 - 詳細
RRC ID | 65439 |
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著者 | Yokomatsu T, Takechi H, Akiyama T, Shibuya S, Kominato T, Soeda S, Shimeno H. |
タイトル | Synthesis and evaluation of a difluoromethylene analogue of sphingomyelin as an inhibitor of sphingomyelinase. |
ジャーナル | Bioorg Med Chem Lett |
Abstract |
A sphingomyelin analogue 2, in which the long alkenyl chain and the phosphodiester moiety of sphingomyelin were replaced by a phenyl and an isosteric difluoromethylenephosphonic acid, was prepared to evaluate its inhibitory potency to sphingomyelinase. The analogue non-competitively inhibited the neutral sphingomyelinase in bovine brain microsomes with an IC50 of 400 microM. The compound had the ability to suppress tumor necrosis factor alpha-induced apoptosis of PC-12 neurons at a low concentration of 0.1 microM. |
巻・号 | 11(10) |
ページ | 1277-80 |
公開日 | 2001-5-21 |
DOI | 10.1016/s0960-894x(01)00179-2 |
PII | S0960894X01001792 |
PMID | 11392536 |
MeSH | Animals Apoptosis / drug effects Brain Cattle Enzyme Inhibitors / chemical synthesis Enzyme Inhibitors / pharmacology Inhibitory Concentration 50 Microsomes / enzymology Neurons / cytology Neurons / drug effects Organophosphonates / chemical synthesis Organophosphonates / pharmacology PC12 Cells Rats Sphingomyelin Phosphodiesterase / antagonists & inhibitors* Sphingomyelins / chemical synthesis* Sphingomyelins / pharmacology Tumor Necrosis Factor-alpha / pharmacology |
IF | 2.572 |
リソース情報 | |
ヒト・動物細胞 | PC-12(RCB0009) |