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

页码：1397 / 1400

页数：4

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