title: Transcription-inhibition and antitumor activities of N-alkylated tetraazacyclododecanes.
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 IC50 values towards HeLa cells in the low-micromolar range.
authors: College of Chemistry & Molecular Sciences, Wuhan University, Wuhan, Hubei 430072, PR China.
authors: Xiao-Qin
authors: XQ
authors: Xiong
authors: Feng
authors: F
authors: Liang
authors: Li
authors: L
authors: Yang
authors: Xiao-Lin
authors: XL
authors: Wang
authors: Xiang
authors: X
authors: Zhou
authors: Cong-Yi
authors: CY
authors: Zheng
authors: Xiao-Ping
authors: XP
authors: Cao
mesh_terms: D000478:Alkylation / Q000187:drug effects; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001372:Aza Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D009369:Neoplasms / Q000235:genetics / Q000473:pathology*; D012333:RNA, Messenger / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship; D014158:Transcription, Genetic / Q000187:drug effects*
chemical_list: D000970:Antineoplastic Agents; D001372:Aza Compounds; D012333:RNA, Messenger