立体化学对放射性金属配合物体内稳定性的影响。2-(对硝基苄基)-反式环二胺四乙酸四种立体异构体的合成与评价。

Stereochemical influence on the stability of radio-metal complexes in vivo. Synthesis and evaluation of the four stereoisomers of 2-(p-nitrobenzyl)-trans-CyDTPA.

作者信息

Wu C, Kobayashi H, Sun B, Yoo T M, Paik C H, Gansow O A, Carrasquillo J A, Pastan I, Brechbiel M W

机构信息

Section, Radiation Oncology Branch, NCI, NIH, Bethesda, MD 20892-1002, USA.

出版信息

Bioorg Med Chem. 1997 Oct;5(10):1925-34. doi: 10.1016/s0968-0896(97)00130-2.

DOI:10.1016/s0968-0896(97)00130-2

PMID:9370037

Abstract

Distinct differences in in vivo stability of the two diastereomeric C-Functionalized CyDTPA chelating agents, (CHX-A DTPA and CHX-B DTPA, both racemates), as recently reported prompted further investigation as to why differences in configuration produced striking effects on the in vivo stability of their yttrium complexes. To this end, the four individual component stereoisomers of CHX-A and CHX-B were synthesized and ability to bind yttrium was investigated both in vitro and in vivo.

摘要

最近报道的两种非对映体C-官能化环二胺四乙酸螯合剂（CHX-A DTPA和CHX-B DTPA，均为外消旋体）在体内稳定性上的明显差异促使人们进一步研究为什么构型差异会对其钇配合物的体内稳定性产生显著影响。为此，合成了CHX-A和CHX-B的四种单个组分立体异构体，并在体外和体内研究了它们结合钇的能力。