Transcription-Inhibition and Antitumor Activities of N-Alkylated Tetraazacyclododecanes

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‐ac...

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Bibliographic Details
Published in:Chemistry & biodiversity 2007-12, Vol.4 (12), p.2791-2797
Main Authors: Xiong, Xiao-Qin, Liang, Feng, Yang, Li, Wang, Xiao-Lin, Zhou, Xiang, Zheng, Cong-Yi, Cao, Xiao-Ping
Format: Article
Language:English
Subjects:
Alkylation - drug effects
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Antitumor activity
Aza Compounds - chemical synthesis
Aza Compounds - chemistry
Aza Compounds - pharmacology
HeLa Cells
Humans
Inhibitors
Inhibitory Concentration 50
Molecular Structure
Neoplasms - genetics
Neoplasms - pathology
Polyamines
RNA, Messenger - genetics
RNA, Messenger - metabolism
Structure-Activity Relationship
Tetraazacyclododecanes
Transcription inhibition
Transcription, Genetic - drug effects
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Summary: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 IC50 values towards HeLa cells in the low‐micromolar range.
ISSN:1612-1872
1612-1880
DOI:10.1002/cbdv.200790228