A new biotin derivative-DOTA conjugate as a candidate for pretargeted diagnosis and therapy of tumors

被引：38

作者：

Sabatino, G

Chinol, M

Paganelli, G

Papi, S

Chelli, M

Leone, G

Papini, AM

De Luca, A

Ginanneschi, M

机构：

[1] Univ Florence, Dept Organ Chem Ugo Schiff, I-50019 Sesto Fiorentino, FI, Italy

[2] ICCOM, CNR, I-50019 Sesto Fiorentino, FI, Italy

[3] European Inst Oncol, Div Nucl Med, I-20141 Milan, Italy

[4] Sigma Tau Ind Farmaceut Riunite SpA, I-00040 Pomezia, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 14期

关键词：

D O I：

10.1021/jm030789z

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of a new biotin derivative, the (CO) reduced N-aminohexyl biotinamido derivative, designed to be serum biotinidase resistant, and its conjugation to the chelator DOTA through an amide bond at one of the four carboxymethyl chains are described. The Y-90-labeled conjugate was able to bind avidin at different Av/conjugate molar ratios with good results. The preclinical results indicate that this new biotin-DOTA conjugate is a good candidate for pretargeted diagnosis and therapy of tumors.

引用

页码：3170 / 3173

页数：4

共 21 条

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