Chiral specificity of novel platinum complexes in their cross-membrane transport and DNA molecular recognition

被引：0
|
作者：
Yang, M [1 ]
Hu, QY [1 ]
Zhang, LR [1 ]
Zhu, SM [1 ]
Zou, J [1 ]
Li, RC [1 ]
Wang, K [1 ]
机构：
[1] Beijing Med Univ, Natl Res Labs Nat & Biomimet Drugs, Beijing 100083, Peoples R China
来源：
SOUTH AFRICAN JOURNAL OF CHEMISTRY-SUID-AFRIKAANSE TYDSKRIF VIR CHEMIE | 1997年 / 50卷 / 04期
关键词：
D O I：
暂无
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
A series of new chiral Pt-complexes has been designed and synthesised. The effects of the chiral features and stereochemistry of newly-synthesised complexes on their anticancer activity, cross-membrane transport and DNA molecular recognition have been studied. The effects of chiral specificity on the cross-membrane transport of Pt-complexes were monitored by measuring the platinum concentration in the cytosol as a function of time. Specific interaction of DNA with three different chiral complexes were investigated by biomicrocalorimetric and CD techniques, and DNA T-m measurements. R,R-Pt was found to be the most active in its cross-membrane transport and its interaction with DNA, which agreed with results in the anticancer tests in vitro. Direct evidence for molecular mechanism of DNA specificity of chiral Pt-complexes was found by HPLC elucidated by molecular modelling studies.
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页码：227 / 231
页数：5
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