Synthesis of hybrid distamycin-cysteine labeled with 99mTc:: a model for a novel class of cancer imaging agents

被引：11
|
作者：
Baraldi, PG [1 ]
Romagnoli, R
Duatti, A
Bolzati, C
Piffanelli, A
Bianchi, N
Mischiati, C
Gambari, R
机构：
[1] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy
[2] Univ Ferrara, Dipartimento Med Clin & Sperimentale, Nucl Med Lab, I-44100 Ferrara, Italy
[3] Univ Ferrara, Diprtimento Biochim & Biol Mol, I-44100 Ferrara, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 12期
关键词：
D O I：
10.1016/S0960-894X(00)00250-X
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis of a hybrid constituted by distamycin A and cysteine labeled with the gamma-emitting radionuclide Tc-99m to afford the conjugate complex 5 is reported, This new radiopharmaceutical is of potential interest as tumor imaging agent in diagnostic nuclear medicine. The preparation of the hybrid distamycin A-cysteine 4 has been achieved by coupling deformyldistamycin A and Boc-Dmt-OH. Compound 4 was then successfully labeled with Tc-99m by reaction with the novel, high-electrophilic, metal-containing fragment [Tc-99m(N)(PP)](2+) (PP = diphosphine ligand) yielding the 1:1 complex 5. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1397 / 1400
页数：4
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