Improved synthesis of the bifunctional chelating agent 1,4,7,10-tetraaza-N-(1-carboxy-3-(4-nitrophenyl)propyl)-N′,N",N′"-tris(acetic acid)cyclododecane (PA-DOTA)

被引：38

作者：

Chappell, LL

Rogers, BE

Khazaeli, MB

Mayo, MS

Buchsbaum, DJ

Brechbiel, MW ^{[1
]}

机构：

[1] NCI, Radioimmune & Inorgran Chem Sect, DCS, NIH, Bethesda, MD 20892 USA

[2] Univ Alabama, Dept Radiat Oncol, Birmingham, AL 35294 USA

[3] Univ Alabama, Dept Med, Birmingham, AL 35294 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1999年 / 7卷 / 11期

关键词：

DOTA; lutetium-177; radioimmono-conjugate; biodistribution;

D O I：

10.1016/S0968-0896(99)00171-6

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A concise synthesis of the bifunctional chelating agent 1,4,7,10-tetraaza-N-(1-carboxy-3-(4-nitrophenyl)propyl)N',N ",N'''-tris(acetic acid)cyclododecane (PA-DOTA) is reported. Difficulties involving the production of partially alkylated products and their removal have been addressed and obviated. After the purl nitro form of PA-DOTA was obtained, conversion to the isothiocyanato form PA-DOTA (1, conjugation to HuCC49 and HuCC49 Delta CH2 monoclonal antibodies was achieved. Subsequent radiolabeling with (LU)-L-177 was performed, demonstrating a useful bifunctional chelating agent suitable for clinical radio-immnunotherapy applications. (C) 1999 Published by Elsevier Science Ltd. All rights reserved.

引用

页码：2313 / 2320

页数：8

共 31 条

[1]

ALVAREZ RD, 1997, GYNENCOLOGIC ONCOLOG, V47, P1185

[2] BACKBONE-SUBSTITUTED DTPA LIGANDS FOR Y-90 RADIOIMMUNOTHERAPY [J].