Mono-(L)-aspartylchlorin-e6
Mono-(L)-aspartylchlorin-e6
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DOI：
10.1111/j.1751-1097.2007.00092.x
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发表时间：
2007-09-01
影响因子：
3.3
通讯作者：
Smith, Kevin M.
中科院分区：
文献类型：
--
作者：
Hargus, Jodie A.;Fronczek, Frank R.;Smith, Kevin M.
Mono-（L）-乙酰二氯-e（6）（也称为他拉泊芬、NPe 6、MACE，最近称为LS-11）是目前正在进行临床试验的用于光动力疗法的有效敏化剂。使用脱镁叶绿素-a和脱镁叶绿酸-a甲酯的明确部分合成、NMR光谱和单晶X-射线衍射的组合，单-（L）-脱镁酰二氢卟酚-e（6）的结构明确地显示为其中脱镁酰残基连接在15（2）-侧链位置的异构体。这一结论与先前的假设相反，但肯定了基于NMR光谱的研究结论;提出了15（2）-藜芦基衍生物独特形成的基本原理。
Mono-(L)-aspartylchlorin-e(6) (also known as Talaporfin, NPe6, MACE, and most recently LS-11) is a potent sensitizer for photodynamic therapy that is currently undergoing clinical trials. Using a combination of unambiguous partial synthesis from pheophytin-a and methyl pheophorbide-a, NMR spectroscopy, and single crystal X-ray diffraction, the structure of mono-(L)-aspartylchlorin-e(6) is definitively shown to be the isomer in which the aspartyl residue is attached at the 15(2)-side chain position. This conclusion is contrary to earlier assumptions, but affirms the conclusions of a study based on NMR spectroscopy; a rationale for the unique formation of the 15(2)-aspartyl derivative is proposed.