期刊
BIOCONJUGATE CHEMISTRY
卷 20, 期 1, 页码 78-86出版社
AMER CHEMICAL SOC
DOI: 10.1021/bc8003183
关键词
-
类别
资金
- Department of Defense [W81XWH0510556]
- Department of Energy Radiochemistry Education [DEFG20705ID14-692IDNE006]
- Washington State University
- M. J. Murdock Charitable Trust
- NSF-EPSCoR
Androgen receptors are overexpressed in most primary and metastatic prostate cancers. A series of single photon emission computed tomography imaging agents (SPECT) utilizing the organometallic radioactive imaging species, fac-Tc-99m(OH2)(3)(CO)(3)(+), were prepared on the basis of the structure of Flutamide, a potent nonsteroidal antiandrogen prostate cancer drug. Novel bifunctional chelate-linked Flutamide analogues were prepared using a newly developed universal alkylating reagent, 2-bromo-N-[4-nitro-3-(trifluoromethyl)phenyl]-acetamide, 1. From compound 1, several ligands (i.e., cysteine 2, histidine 5, imidazole 3) were conjugated to the flutamide derivative to yield targeting ligands capable of either tridentate or monodentate coordination in a 2 + 1 complex. fac-Re(CO)(3)(+) complexes were prepared and characterized with the functionalized conjugates to yield fac-Re(CO)(3)(2-amino-3-(1-(2-(4-nitro-3-(trifluoromethyl)phenylamino)-2-oxoethyl)-1H-imidazol-4-yl)propanoate), 4,fac-Re (CO)(3)(2-(S-cysteinyl)-N-[4-nitro-3-(trifluoromethyl) phenyl]-acetamide), 6, and fac-Re(CO)(3)(picolinate)(2-(1H-imidazol-1-yl)-N-[4-nitro-3-(trifluoromethyl)phenyl]-acetamide), 7. The corresponding radioactive Tc-99m analogues were prepared and stability studies of the radioactive compounds were also conducted.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据