Simplified dynemicin analogues: diastereoselective synthesis and evaluation of their activity against plasmid DNA

被引:16
作者
Guanti, G [1 ]
Riva, R [1 ]
机构
[1] Dipartimento Chim & Chim Ind, I-16146 Genoa, Italy
关键词
D O I
10.1039/b307966j
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The total synthesis of two diastereoisomeric simplified dynemicin analogues is reported. The key steps involved are: the regio- and diastereoselective functionalisation of an appropriate racemic quinoline precursor and the ring closure to give the 10-membered enediyne moiety through a Pd(0)-catalysed Stille reaction. After the successful conversion of one of these derivatives into a compound more readily activable under nearly physiological conditions, the activity against plasmid DNA was evaluated.
引用
收藏
页码:3967 / 3976
页数:10
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