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Transcription‐Inhibition and Antitumor Activities of N ‐Alkylated Tetraazacyclododecanes
Author(s) -
Xiong XiaoQin,
Liang Feng,
Yang Li,
Wang XiaoLin,
Zhou Xiang,
Zheng CongYi,
Cao XiaoPing
Publication year - 2007
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.200790228
Subject(s) - hela , chemistry , transcription (linguistics) , in vitro , alkyl , alkylation , stereochemistry , rna polymerase ii , rna polymerase , structure–activity relationship , rna , biological activity , biochemistry , microbiology and biotechnology , gene , gene expression , organic chemistry , biology , promoter , linguistics , philosophy , catalysis
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.