Synthesis and Cytotoxic Activity of New Vindoline Derivatives Coupled to Natural and Synthetic Pharmacophores

与天然和合成药效团偶联的新型文多林衍生物的合成及细胞毒活性

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作者:András Keglevich, Leonetta Dányi, Alexandra Rieder, Dorottya Horváth, Áron Szigetvári, Miklós Dékány, Csaba Szántay Jr, Ahmed Dhahir Latif, Attila Hunyadi, István Zupkó, Péter Keglevich, László Hazai

Abstract

New Vinca alkaloid derivatives were synthesized to improve the biological activity of the natural alkaloid vindoline. To this end, experiments were performed to link vindoline with various structural units, such as amino acids, a 1,2,3-triazole derivative, morpholine, piperazine and N-methylpiperazine. The structure of the new compounds was characterized by NMR spectroscopy and mass spectrometry (MS). Several compounds exhibited in vitro antiproliferative activity against human gynecological cancer cell lines with IC50 values in the low micromolar concentration range.

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