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Synthesis and Human Anticancer Cell Line Studies on Coumarin-β-carboline Hybrids as Possible Antimitotic Agents

机译:合成和人类抗癌细胞系研究香豆素 - β-果酸酯杂种,可能是抗染色体

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摘要

A series of coumarin tetrahydro-β-carboline hybrids 3 have been synthesized by the Pictet-Spengler reaction. Stoichio- metrically controlled DDQ oxidation has led to dihydro 4 and β- carboline 5. In vitro anticancer activity against 60 cell lines has revealed the potency of 3f, 4a and 5c. In silico studies indicate the binding properties of 5c with Kinesin spindle protein (KSP) and tubulin protein. Gel electrophoresis studies revealed that compound 3f partially cleaved the CT-DNA, whereas the ring C aromatized compound 5c completely cleaved the CT-DNA. Structures of the newly synthesized compounds are confirmed by spectroscopic and X-ray studies.
机译:一系列香豆素四氢-β-碳纤维蛋白杂交3已通过Pictet-Spenger反应合成。 石化控制的DDQ氧化导致了二氢4和β-碳纤维蛋白5.对60个细胞系的体外抗癌活性揭示了3F,4A和5C的效力。 在计算机研究中表明,5C与驱动蛋白纺锤体蛋白(KSP)和微管蛋白蛋白具有结合特性。 凝胶电泳研究表明,化合物3F部分裂解了CT-DNA,而环C芳香化合物5C完全裂解了CT-DNA。 新合成化合物的结构通过光谱和X射线研究证实。

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