A comparative study of trans- and cis-isomers of a bone-seeking agent, DO2A2P.
A comparative study of trans- and cis-isomers of a bone-seeking agent, DO2A2P.
复制标题
寻骨剂 DO2A2P 反式和顺式异构体的比较研究。
DOI：
10.1016/j.bmcl.2014.12.016
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发表时间：
2015
影响因子：
2.7
通讯作者：
Sun,Xiankai
中科院分区：
文献类型：
--
作者：
Hao,Guiyang;Liu,Wei;Hassan,Gedaa;Öz,OrhanK;Kovacs,Zoltan;Sun,Xiankai
该大环寻骨剂DO2A2P含有一个环素核心和两对外围的膦酸基和羧酸基。外围官能团的几何配置产生了一对几何异构体：顺式-DO2A2P和反式-DO2A2P。为了比较异构体对的生物学行为，合成了顺式DO2A2P。这两种异构体都被成功地用~(177)Lu标记，这可能会加强它们在放射治疗和骨疾病成像中的应用。通过一系列生物学测试，包括羟基磷灰石结合、体外稳定性和体内分布，我们证明了DO2A2P几何对具有几乎相同的生物学特性。
The macrocyclic bone-seeking agent, DO2A2P, bears a cyclen core and two pairs of peripheral phosphonate and carboxylate groups. The geometric disposition of the peripheral functionalities gives arise to a pair of geometric isomers:cis-DO2A2P andtrans-DO2A2P. In order to compare the biological behavior of the isomer pair,cis-DO2A2P was synthesized. Both isomers were successfully radiolabeled with177Lu, which might potentiate their applications in both radiotherapy and imaging of bone diseases. Through a set of biological assays including the hydroxyapatite binding, in vitro stability, and in vivo distribution, we demonstrated that the geometric pair of DO2A2P had virtually identical biological properties.