Journal of Medicinal Chemistry p. 1127 - 1134 (1989)
Update date:2022-08-05
Topics:
Dodin, G.
Ditercalinium, a 7H-pyridocarbazole dimer designed to bisintercalate into DNA, forms tight ion pairs in water with inorganic and organic anions.The thermodynamics and kinetics of the acetate-ditercalinium pairing has been investigated by means of T-juump spectroscopy.The formation of the pair has a constant estimated to 1000 M-1 and proceeds via a fasr two-step mechanism with a relaxation time of 12 μs (acetate pH 5) to 50 μs (cacodylate, pH 7.5) involving an intermediate solvent-separated ion oair.A strong association of ditercalinium to cardiolipid has been observed and is expected to be involved in the respiratory chain inhibitio n induced by ditercalinium (unpublished results).Direct estimates of the binding constants of the drug to calf thymus DNA were obtained by means of UV titrations at high drug/base ratio (>0.17).The maximum number of binding sites per base both at pH 5 and pH 7.5 was found to be 0.22, a value consistent with monointercalation as expected from the prediction of Shafer's model for the interaction of bifunctional ligands to DNA.This work also supports the hypothesis that significant ionic binding may account for the ditercalinium/DNA interaction at high base/drug ratios (0.2).
View MoreContact:86 21 3772 9386
Address:Rm.1803,Starry Bldg.1,1505 Meijiabang Road,Shanghai 201620 China
Shanghai Dynamic Industrial Co.,Ltd.
website:http://www.shdynamic.com
Contact:86-021 3392 6680
Address:Room 805 Information Tower, No.1403 Minsheng Road, Pudong New Area, Shanghai 200135, P. R. China
Contact:18698110882
Address:1303 No2 building,LuoMa Garden,YongAn Road,Hexi District,Tianjin city
Shandong Jincheng Zhonghua Bio-pharmaceutical Co.,Ltd
Contact:+86-533-5415882
Address:Zichuan Economic Development Zone,Zibo City,Shandong Province,China
Contact:+86+21-58956006 15800617331
Address:402 Room, 150# Cailun Road, Zhangjiang high tech park, Shanghai
Doi:10.1016/j.tet.2017.02.055
(2017)Doi:10.1016/S0040-4039(00)85316-2
(1986)Doi:10.1246/bcsj.53.1010
(1980)Doi:10.1016/j.mcat.2018.01.026
(2018)Doi:10.1021/ja01191a049
(1948)Doi:10.1016/S0020-1693(00)88425-X
(1980)