新型长春多灵衍生物与天然及合成药效基团偶联物的合成及细胞毒性活性

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

作者信息

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

机构信息

Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, H-1111 Budapest, Gellért tér 4., Hungary.

Spectroscopic Research Department, Gedeon Richter Plc., H-1475 Budapest 10, P. O. Box 27, Hungary.

出版信息

Molecules. 2020 Feb 24;25(4):1010. doi: 10.3390/molecules25041010.

New 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 IC values in the low micromolar concentration range.