Configurationally restricted bismacrocyclic CXCR4 receptor antagonists
Configurationally restricted bismacrocyclic CXCR4 receptor antagonists
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DOI：
10.1021/jm0607810
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发表时间：
2006-10-19
影响因子：
7.3
通讯作者：
Archibald, Stephen J.
中科院分区：
文献类型：
--
作者：
Valks, Gina C.;McRobbie, Graeme;Archibald, Stephen J.
合成了一种含锌（II）的双大环cyclam型CXCR 4趋化因子受体拮抗剂的构型限制类似物，并显示其在溶液中仅采用一种构型。单晶X-射线结构揭示了有利的结合，通过双齿螯合，可以与受体蛋白表面上的天冬氨酸的相互作用。锌（II）络合物在体外对HIV感染具有高度活性。
A zinc(II) containing configurationally restricted analogue of bismacrocyclic cyclam-type CXCR4 chemokine receptor antagonists has been synthesized and shown to adopt only one configuration in solution. The single crystal X-ray structure reveals favorable binding to acetate via a bidentate chelation that can be related to the proposed interaction with aspartate on the receptor protein surface. The zinc(II) complex is highly active against HIV infection in vitro.