Molecules
(Feb 2020)
Synthesis and Cytotoxic Activity of New Vindoline Derivatives Coupled to Natural and Synthetic Pharmacophores
András Keglevich,
Leonetta Dányi,
Alexandra Rieder,
Dorottya Horváth,
Áron Szigetvári,
Miklós Dékány,
Csaba Szántay,
Ahmed Dhahir Latif,
Attila Hunyadi,
István Zupkó,
Péter Keglevich,
László Hazai
Affiliations
András Keglevich
Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Gellért tér 4., H-1111 Budapest, Hungary
Leonetta Dányi
Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Gellért tér 4., H-1111 Budapest, Hungary
Alexandra Rieder
Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Gellért tér 4., H-1111 Budapest, Hungary
Dorottya Horváth
Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Gellért tér 4., H-1111 Budapest, Hungary
Áron Szigetvári
Spectroscopic Research Department, Gedeon Richter Plc., P. O. Box 27, H-1475 Budapest 10, Hungary
Miklós Dékány
Spectroscopic Research Department, Gedeon Richter Plc., P. O. Box 27, H-1475 Budapest 10, Hungary
Csaba Szántay
Spectroscopic Research Department, Gedeon Richter Plc., P. O. Box 27, H-1475 Budapest 10, Hungary
Ahmed Dhahir Latif
Institute of Pharmacognosy, Interdisciplinary Excellence Centre, University of Szeged, Eötvös u. 6., H-6720 Szeged, Hungary
Attila Hunyadi
Institute of Pharmacognosy, Interdisciplinary Excellence Centre, University of Szeged, Eötvös u. 6., H-6720 Szeged, Hungary
István Zupkó
Department of Pharmacodynamics and Biopharmacy, Interdisciplinary Excellence Centre, University of Szeged, Eötvös u. 6., H-6720 Szeged, Hungary
Péter Keglevich
Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Gellért tér 4., H-1111 Budapest, Hungary
László Hazai
Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Gellért tér 4., H-1111 Budapest, Hungary
DOI
https://doi.org/10.3390/molecules25041010
Journal volume & issue
Vol. 25,
no. 4
Abstract
Read online
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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