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Clathrochelate complexes as promising molecular scaffolds for novel biomimetic systems, (radio) pharmaceuticals and topological drugs

机译:Clathrochelate复合物作为新型生物摩擦系统的有前途的分子支架,(无线电)药物和拓扑药物

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The applicability of the clathrochelates as the biomimetic systems, (radio)pharma-ceuticals and topological drugs as well as an inhibition of the model enzymes (RNA polymerase and topoisomerase) by these complexes are discussed.The modern approach to the pharmaceutical screening is based on several paradigms and empirical rules. They limit the chemical compounds that have a potential as pharmaceuticals for diagnostics and therapy; many chemical systems and classes have been excluded from the routine screening studies and, therefore, are terra incognita for biochemists, pharmacologists, and clinicians. For example, one of the Lipinski's rules [1] states that the molecular weight of the chemical compounds that can be used for pharmaceutical screening should be under 500 Da. The biological activity of these low-weight compounds, constituting up to 90% of the pharmaceutical market (by nomenclature), in most cases is governed by their interactions with biological targets via either covalent or supramolecular bonding.
机译:讨论了Clathrochelate作为仿生系统的适用性,(无线电)药气和拓扑药物以及这些配合物的模型酶(RNA聚合酶和拓扑异构酶)的抑制作用。药物筛查的现代方法是基于几个范例和经验规则。它们限制了具有诊断和治疗药物的潜力的化学化合物;许多化学系统和课程被排除在常规筛查研究之外,因此,生物化学师,药剂学家和临床医生的Terra Incognita。例如,Lipinski的规则之一[1]指出可用于药物筛选的化合物的分子量应在500 da下。在大多数情况下,这些低重量级化合物的生物学活性高达90%的药物市场(通过命名),通过它们与生物靶标的相互作用来控制通过共价或超分子键合。

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