Design, synthesis, and evaluation of cyclofenil derivatives for potential SPECT imaging agents.
To develop technetium- and rhenium-labeled nonsteroidal estrogen imaging agents for estrogen receptor (ER) positive breast tumors, two groups of rhenium and technetium cyclofenil derivatives were synthesized and characterized. The binding affinities of the rhenium complexes for ERs were determined. The tricarbonyl rhenium complex showed the highest binding affinity for ERs (81.2 for ERbeta, 16.5 for ERalpha). Tricarbonyl technetium cyclofenil complexes were obtained in high radiochemical purity and radiochemical yields. The results of studies of their octanol/water partition and in vitro stability are presented. These results demonstrate that these radiolabeled cyclofenil derivatives may be considered as potential breast cancer imaging agents.
Zhu
Hua
H
Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai, 201800, China.
Huang
Liliang
L
Zhang
Yuanqing
Y
Xu
Xiaoping
X
Sun
Yanhong
Y
Shen
Yu-Mei
YM
D001943:Breast Neoplasms / Q000000981:diagnostic imaging / Q000378:metabolism; D003506:Cyclofenil / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D015195:Drug Design; D004355:Drug Stability; D006801:Humans; D008024:Ligands; D000442:Octanols / Q000737:chemistry; D015609:Organotechnetium Compounds / Q000737:chemistry; D011960:Receptors, Estrogen / Q000378:metabolism; D012211:Rhenium; D015899:Tomography, Emission-Computed, Single-Photon; D014867:Water / Q000737:chemistry
D008024:Ligands; D000442:Octanols; D015609:Organotechnetium Compounds; D011960:Receptors, Estrogen; D014867:Water; D012211:Rhenium; D003506:Cyclofenil