机构：[1]Medical Imaging Key Laboratory of Sichuan Province, Department of Oncology, Affiliated Hospital of North Sichuan Medical College, Nanchong 637000, Sichuan, China.[2]School of Basic Medical Sciences and Forensic Medicine, North Sichuan Medical College, Nanchong 637000, Sichuan, China.[3]School of Pharmacy, North Sichuan Medical College, Nanchong 637000, Sichuan, China.[4]Key Laboratory of Synthetic and Self-Assembly Chemistry for Organic Functional Molecules, Center for Excellence in Molecular Synthesis, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 200032, China.[5]State Key Laboratory of Organometallic Chemistry and Shanghai Hongkong Joint Laboratory in Chemical Synthesis Key Laboratory of Synthetic and Self-Assembly Chemistry for Organic Functional Molecules, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 200032, China.
A novel Fe(III) complex, Fe-tBPCDTA, was synthesized and explored as a potential contrast agent for MRI. Compared to established agents like Fe-EDTA and Fe-tCDTA, Fe-tBPCDTA exhibited moderate relaxivity (r1 = 1.17 s-1·mmol-1) due to its enhanced second-sphere mechanism. It also displayed improved kinetic inertness, lower cytotoxicity, and enhanced redox stability. In vivo studies demonstrated its function as an extracellular fluid agent, providing tumor contrast comparable to that of Gd-DTPA at a higher dosage. Complete renal clearance occurred within 24 h. These findings suggest Fe-tBPCDTA as a promising candidate for further development as a safe and effective extracellular MRI contrast agent.
基金：
This research was made possible as a result of a generous grant
from the National Natural Science Foundation of China
(81671675, 21172025) and the Science and Technology
Project of Municipal School Strategic Cooperation, Nanchong
(NSMC20170101, 18SXHZ0091, 18SXHZ0379,
20SXQT0180, CBY23-QDA09). Prof. Dr. J. Tian acknowledges the funding support from the National Natural Science
Foundation of China (22271306), the Strategic Priority
Research Program of the Chinese Academy of Sciences
(XDB0610000), and the Shanghai Rising-Star Program
(22QA1411200).
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2024]版：
无
最新[2023]版：
大类|1 区医学
小类|1 区药物化学
第一作者：
第一作者机构：[1]Medical Imaging Key Laboratory of Sichuan Province, Department of Oncology, Affiliated Hospital of North Sichuan Medical College, Nanchong 637000, Sichuan, China.[2]School of Basic Medical Sciences and Forensic Medicine, North Sichuan Medical College, Nanchong 637000, Sichuan, China.
共同第一作者：
通讯作者：
推荐引用方式(GB/T 7714)：
He Ling,Wang Haiyu,Zeng Zuhua,et al.Rigid Fe(III) Chelate with Phosphonate Pendants: A Stable and Effective Extracellular MRI Contrast Agent[J].Journal Of Medicinal Chemistry.2024,doi:10.1021/acs.jmedchem.3c02338.
APA：
He Ling,Wang Haiyu,Zeng Zuhua,Zhong Lei,Tang Qingxuan...&Zhu Jiang.(2024).Rigid Fe(III) Chelate with Phosphonate Pendants: A Stable and Effective Extracellular MRI Contrast Agent.Journal Of Medicinal Chemistry,,
MLA：
He Ling,et al."Rigid Fe(III) Chelate with Phosphonate Pendants: A Stable and Effective Extracellular MRI Contrast Agent".Journal Of Medicinal Chemistry .(2024)
医学