EFFECT OF LINKER LENGTH ON DNA-BINDING AFFINITY, CROSS-LINKING EFFICIENCY AND CYTOTOXICITY OF C8-LINKED PYRROLOBENZODIAZEPINE DIMERS

被引：75

作者：

BOSE, DS

THOMPSON, AS

SMELLIE, M

BERARDINI, MD

HARTLEY, JA

JENKINS, TC

NEIDLE, S

THURSTON, DE

机构：

[1] UNIV PORTSMOUTH,SCH PHARM & BIOMED SCI,DIV MED CHEM,KING HENRY 1ST ST,PORTSMOUTH PO1 2DZ,ENGLAND

[2] UNIV COLL & MIDDLESEX SCH MED,DEPT ONCOL,LONDON W1P 8BT,ENGLAND

[3] INST CANC RES,BIOMOLEC STRUCT UNIT,CANC RES CAMPAIGN,SUTTON SM2 5NG,ENGLAND

来源：

JOURNAL OF THE CHEMICAL SOCIETY-CHEMICAL COMMUNICATIONS | 1992年 / 20期

关键词：

D O I：

10.1039/c39920001518

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

An efficient synthesis of a homologous series of C8-linked pyrrolobenzodiazepine dimers is reported; compounds with an odd number of methylenes (n = 3 or 5) in the linker show a higher affinity for DNA, enhanced cross-linking efficiency, and are more cytotoxic compared with compounds with either n = 4 or 6.

引用

收藏

页码：1518 / 1520

页数：3

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