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Transcription-Inhibition and Antitumor Activities of N-Alkylated Tetraazacyclododecanes

✍ Scribed by Xiao-Qin Xiong; Feng Liang; Li Yang; Xiao-Lin Wang; Xiang Zhou; Cong-Yi Zheng; Xiao-Ping Cao


Book ID
101773414
Publisher
John Wiley and Sons
Year
2007
Tongue
English
Weight
241 KB
Volume
4
Category
Article
ISSN
1612-1872

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✦ Synopsis


Abstract

A series of alkyl‐substituted tetraazacyclododecane congeners were synthesized, and their antitumor activities towards human HeLa cells as well as their effect on the in vitro transcription with T7 RNA polymerase were investigated. A structure–activity‐relationship (SAR) study identified the most‐active congeners as those with medium alkyl‐chain lengths. Three compounds, 57, were found to exhibit significant biological activities, with IC~50~ values towards HeLa cells in the low‐micromolar range.


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