Design and synthesis of dimeric HIV-1 integrase inhibitory peptides

被引：26

作者：

Krajewski, K

Long, YQ

Marchand, C

Pommier, Y

Koller, PP ^{[1
]}

机构：

[1] NCI Frederick, CCR, Med Chem Lab, NIH, Frederick, MD 21702 USA

[2] Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 200031, Peoples R China

[3] NCI, Mol Pharmacol Lab, CCR, NIH, Bethesda, MD 20892 USA

[4] Univ Wroclaw, Fac Chem, PL-50383 Wroclaw, Poland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(03)00679-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Dimers of known HIV-1 integrase inhibitory hexapeptide H-His-Cys-Lys-Phe-Trp-Trp-NH2 containing different lengths of cross linkers in the place of cysteine residue, were designed, and synthesized. The inhibitory potency of these dimeric peptides is consistently higher than the lead hexapeptide. The dimeric peptide with djenkolic acid linker exhibited IC50 values of 5.3 and 6.5 muM, for 3'-end processing and strand transfer, respectively. (C) 2003 Elsevier Ltd. All rights reserved.

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页码：3203 / 3205

页数：3

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