Synthesis and biological studies of N-alkylated cyclic diamines.
Several alkyl-substituted mesocyclic diamines were synthesized, and their interaction with DNA were studied by melting-temperature measurements and the ethidium bromide (EB)-fluorescence competitive method. The supercoiled DNA hydrolytic cleavage by 1,4-dioctyl-1,4-diazepan-6-ol (4) was supported by the evidence from free-radical quenching and T4-ligase ligation. Preliminary pharmacological tests showed that only 1,4-dioctyl-1,4-diazepan-6-ol (4) had antitumor activity against HeLa cell lines in vitro.
Xiong
Xiao-Qin
XQ
College of Chemistry & Molecular Sciences, Wuhan University, Wuhan, Hubei 430072, PR China.
Liang
Feng
F
Yang
Li
L
Zhou
Xiang
X
Zheng
Cong-Yi
CY
Cao
Xiao-Ping
XP
D000478:Alkylation; D003500:Cyclization; D004247:DNA / Q000187:drug effects* / Q000378:metabolism; D003959:Diamines / Q000138:chemical synthesis* / Q000494:pharmacology*; D006367:HeLa Cells; D006801:Humans; D006868:Hydrolysis; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization
D003959:Diamines; D004247:DNA