Gniazdowski M, Szmigiero L, Wilmańska D
Cancer Lett. 1982 Jan;15(1):73-9. doi: 10.1016/0304-3835(82)90078-7.
In the presence of sulfhydryl compounds an anticancer drug, 1-nitro-9-aminoalkylacridine derivative, forms with DNA irreversible, probably covalent, complexes of decreased template properties. Five 9-substituted 1-nitro-9-aminoacridine derivatives of cytostatic activity show irreversible thiol-dependent inhibitory effects on the RNA synthesis in vitro system while equal inhibition is observed both in the presence and in the absence of dithiothreitol with biologically inactive analogues of nitrocrine. In the absence of sulfhydryl compounds the inhibition depends on the planarity of the acridine ring. Hence, both 1-nitro-9-aminoalkylacridine and tetrahydroacridine derivatives show low inhibitory effect.
在巯基化合物存在的情况下，一种抗癌药物1-硝基-9-氨基烷基吖啶衍生物与DNA形成不可逆的（可能是共价的）复合物，其模板性质降低。五种具有细胞抑制活性的9-取代1-硝基-9-氨基吖啶衍生物对体外RNA合成系统表现出不可逆的硫醇依赖性抑制作用，而对于硝基吖啶的无生物学活性类似物，无论有无二硫苏糖醇存在均观察到同等程度的抑制。在没有巯基化合物的情况下，抑制作用取决于吖啶环的平面性。因此，1-硝基-9-氨基烷基吖啶和四氢吖啶衍生物均表现出较低的抑制作用。
