Piestrzeniewicz M K, Czyz M, Denny W A, Gniazdowski M
Department of General Chemistry, Institute of Physiology and Biochemistry, School of Medicine, Lódź, Poland.
Acta Biochim Pol. 1990;37(2):299-307.
A series of 9-aminoacridine carboxamide derivatives of systematically varied structure was assayed in an RNA synthesis in vitro system. Escherichia coli DNA-dependent RNA polymerase and DNA derived from phage T7 or calf thymus were used to measure the effect of the drugs on overall RNA and the initiating dinucleotide (pppApU) syntheses. By means of multiple linear regression analysis it was shown that the inhibition of these reactions depends both on the drug equilibrium binding constant and kinetic parameters of dissociation of drug-DNA complexes.
对一系列结构系统变化的9-氨基吖啶羧酰胺衍生物在体外RNA合成系统中进行了测定。使用大肠杆菌DNA依赖性RNA聚合酶以及来自噬菌体T7或小牛胸腺的DNA来测量这些药物对整体RNA和起始二核苷酸(pppApU)合成的影响。通过多元线性回归分析表明,这些反应的抑制作用既取决于药物的平衡结合常数,也取决于药物 - DNA复合物解离的动力学参数。