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, 5–7, were found to exhibit significant biological activities, with IC~50~ values towards HeLa cells in the low‐micromolar range.
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