Benzene fused monocyclic enediynyl amides: Synthesis, reactivity and DNA-cleavage activity in comparison to the corresponding sulfonamides

被引：30

作者：

Basak, A ^{[1
]}

Mandal, S

Das, AK

Bertolasi, V

机构：

[1] Indian Inst Technol, Dept Chem, Kharagpur 721302, W Bengal, India

[2] Indian Inst Technol, Dept Biotechnol, Kharagpur 721302, W Bengal, India

[3] Univ Ferrara, Dipartimento Chim, I-44100 Ferrara, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(02)00029-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Monocyclic enediynyl amides 2a 2c have been synthesized via the corresponding free amine 5. Kinetic studies in chloroform revealed the reactivity of these amides towards Bergman cyclization to be less than that of the corresponding sulfonamides. However, differential scanning calorimetry (DSC) measurements in the solid state and DNA-cleavage studies in aqueous buffer showed higher reactivity for the amides than the sulphonamides. (C) 2002 Published by Elsevier Science Ltd.

引用

页码：873 / 877

页数：5

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