Improved synthesis and evaluation of 17-substituted aminoalkylgeldanamycin derivatives applicable to drug delivery systems

被引：32

作者：

Kasuya, Y

Lu, ZR

Kopecková, P

Kopecek, J ^{[1
]}

机构：

[1] Univ Utah, Dept Pharmaceut & Pharmaceut Chem, CCCD, Salt Lake City, UT 84112 USA

[2] Univ Utah, Dept Bioengn, Salt Lake City, UT 84112 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(01)00374-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The 17-methoxy group of geldanamycin was substituted with 1,3-diaminopropane and 1,3-diamino-2-hydroxypropane to introduce a primary amino group useful for conjugation with targeting moieties and drug carriers. We have developed a procedure that has provided improved yield and reproducibility of the syntheses. Both geldanamycin derivatives demonstrated antiproliferative activity towards the human ovarian carcinoma cell line, A2780. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：2089 / 2091

页数：3

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