Solid-phase synthesis of acridine-based threading intercalator peptides

被引：45

作者：

Carlson, CB ^{[1
]}

Beal, PA ^{[1
]}

机构：

[1] Univ Utah, Dept Chem, Salt Lake City, UT USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(00)00388-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The preparation of a novel acridine-based amino acid is reported. This N-Alloc-protected monomer call be coupled and deprotected under solid-phase peptide synthesis procedures to create acridine-peptide conjugates as potential threading intercalators. A peptide containing this novel amino acid undergoes spectral changes in the presence of duplex DNA and RNA consistent with intercalative binding. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1979 / 1982

页数：4

共 25 条

[1] Crystal structure of the topoisomerase II poison 9-amino-[N-(2-dimethylamino)ethyl]acridine-4-carboxamide bound to the DNA hexanucleotide d(CGTACG)2 [J].