Synthesis and biological evaluation of novel daunorubicin-estrogen conjugates

被引：37

作者：

Kasiotis, KM

Magiatis, P

Pratsinis, H

Skaltsounis, AL

Abadji, V

Charalambous, A

Moutsatsou, P

Haroutounian, SA

机构：

[1] Agr Univ Athens, Chem Lab, Athens 11855, Greece

[2] Natl Tech Univ Athens, Dept Pharm, Zografos 15771, Greece

[3] Natl Tech Univ Athens, Sch Med, Zografos 15771, Greece

[4] ELPEN SA, Pharmaceut Co, Pikermi 19009, Greece

来源：

STEROIDS | 2001年 / 66卷 / 10期

关键词：

daunorubicin conjugates; steroidal and non-steroidal estrogen ligand; synthesis; estrogen receptor binding; cytotoxic activity;

D O I：

10.1016/S0039-128X(01)00110-6

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：

The synthesis of two novel daunorubicin-estro-en conjugates with a steroidal and a non-steroidal ligand was undertaken in an attempt to target the cytotoxicity of anthracycline to estrogen-receptor positive cells. These conjugates (3 and 4), in contrast to their corresponding ligands, displayed weak binding affinities of 0.079 and 0.851 for the estrogen receptor. Conjugate 3 was consistently more cytotoxic than 4, which however showed some selectivity to estrogen receptor positive cell lines. (C) 2001 Elsevier Science Inc. All rights reserved.

引用

页码：785 / 791

页数：7

共 26 条

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