Synthesis of Pseudomonas quorum-sensing autoinducer analogs and structural entities required for induction of apoptosis in macrophages
Synthesis of Pseudomonas quorum-sensing autoinducer analogs and structural entities required for induction of apoptosis in macrophages
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DOI：
10.1016/j.bmcl.2006.01.054
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发表时间：
2006-04-15
影响因子：
2.7
通讯作者：
Ishiguro, M
中科院分区：
文献类型：
--
作者：
Horikawa, M;Tateda, K;Ishiguro, M
本文报道了N-3-氧代十二烷酰基-L-高丝氨酸内酯类似物(1)的合成及其诱导巨噬细胞P388D1细胞凋亡的构效关系。结果表明，除了L-高丝氨酸内酯单元的存在外，酰基侧链上氧基的位置对其诱导细胞凋亡活性是至关重要的。此外，具有疏水末端的长的酰基侧链更有利于活性。(C)2006爱思唯尔有限公司。保留所有权利。
The synthesis of the analogs of N-3-oxododecanoyl-L-homoserine lactone (1) and their structure-activity relationship for the apoptotic induction in macrophages, P388D1 cells, are described. It was revealed that the position of the oxo group in the acyl side chain in addition to the presence of the L-homoserine lactone unit is crucial for the apoptosis-inducing activity. Furthermore, the long acyl side chains with hydrophobic distal ends are preferable for the activity. (C) 2006 Elsevier Ltd. All rights reserved.