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Electrochemical and calorimetric investigation of interaction of novel biscationic anticancer agents with DNA

机译:新型双阳离子抗癌药物与DNa相互作用的电化学和量热研究

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摘要

Biscationic amidines bind in the DNA minor groove and present biological activity against a range of infectious diseases. Two new biscationic compounds (bis-α,ω-S-thioureido, amino and sulfide analogues) were synthesized in good yields and fully characterized, and their interaction with DNA was also investigated. Isothermal titration calorimetry (ITC) was used to measure the thermodynamic properties of binding interactions between DNA and these ligands. A double stranded calf thymus DNA immobilized on an electrode surface was used to study the possible DNA-interacting abilities of these compounds towards dsDNA in situ. A remarkable interaction of these compounds with DNA was demonstrated and their potential application as anticancer agents was furthered.
机译:双阳离子am结合在DNA小沟中,对多种传染病具有生物学活性。以高收率合成了两种新的双阳离子化合物(双-α,ω-S-硫脲基,氨基和硫化物类似物)并进行了充分表征,并研究了它们与DNA的相互作用。等温滴定热法(ITC)用于测量DNA与这些配体之间结合相互作用的热力学性质。使用固定在电极表面的双链小牛胸腺DNA来研究这些化合物对dsDNA的可能的DNA相互作用能力。这些化合物与DNA具有显着的相互作用,并进一步证明了其作为抗癌剂的潜在应用。

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