Design, synthesis, and preliminary biological evaluation of a novel triazole analogue of ceramide
Design, synthesis, and preliminary biological evaluation of a novel triazole analogue of ceramide
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DOI：
10.1016/j.bmcl.2007.05.086
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发表时间：
2007-08-15
影响因子：
2.7
通讯作者：
Lee, Sang Kook
中科院分区：
文献类型：
--
作者：
Kim, Sanghee;Cho, Minjae;Lee, Sang Kook
神经酰胺的酰胺键被不可水解的1，2，3-三唑官能团取代。采用点击化学合成所设计的类似物。我们的初步生物学评价表明，神经酰胺的酰胺部分是顺从的生物电子等排取代与三唑部分。一些类似物比C2-神经酰胺作为细胞毒性剂更有效，观察到的细胞毒性可能是通过诱导细胞凋亡介导的。(c)2007爱思唯尔有限公司保留所有权利。
The amide bond of ceramide was replaced by the non-hydrolyzable 1,2,3-triazole functionality. Click chemistry was employed for synthesis of the designed analogues. Our preliminary biological evaluation indicated that the amide moiety of ceramide is amenable to bioisosteric substitution with the triazole moiety. Some of the analogues were more potent than C2-ceramide as cytotoxic, agents, and the observed cytotoxicity was possibly mediated through the induction of apoptosis. (c) 2007 Elsevier Ltd. All rights reserved.