Estradiol-mimetic probes.: Preparation of 17α-(6-aminohexynyl)estradiol biotin, fluorescein and acridinium conjugates

被引：14

作者：

Adamczyk, M ^{[1
]}

Chen, YY ^{[1
]}

Moore, JA ^{[1
]}

Mattingly, PG ^{[1
]}

机构：

[1] Abbott Labs, Dept Chem, Div Diagnost, Dept 09NM, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(98)00225-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

3-O-tert-Butyldimethylsilyl-17 alpha-(6-mesyloxyhexynyl)estradiol was converted to the azide in 60-70% yield with NaN3/DMPU, then reduced to the corresponding amine (>95% yield). Acylation with the N-hydroxysuccinimide esters of biotin, 5-carboxyfluorescein and 10-(3-sulfopropyl)-N-tosyl-N-(3-carboxypropyl)acridinium-9-carboxamide gave the title conjugates. The K(D)s of the tracers with an estradiol antibody ranged from 97-197 nM. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1281 / 1284

页数：4

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