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Synthesis and Cytotoxic Activity of New Vindoline Derivatives Coupled to Natural and Synthetic Pharmacophores
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-methylpiperazi...
| Autores principales: | , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
MDPI
2020
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7070384/ https://www.ncbi.nlm.nih.gov/pubmed/32102414 http://dx.doi.org/10.3390/molecules25041010 |
| _version_ | 1783505962727899136 |
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| author | 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 |
| author_facet | 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 |
| author_sort | Keglevich, András |
| collection | PubMed |
| description | 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 IC(50) values in the low micromolar concentration range. |
| format | Online Article Text |
| id | pubmed-7070384 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2020 |
| publisher | MDPI |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-70703842020-03-19 Synthesis and Cytotoxic Activity of New Vindoline Derivatives Coupled to Natural and Synthetic Pharmacophores 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 Molecules Article 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 IC(50) values in the low micromolar concentration range. MDPI 2020-02-24 /pmc/articles/PMC7070384/ /pubmed/32102414 http://dx.doi.org/10.3390/molecules25041010 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
| spellingShingle | Article 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 Synthesis and Cytotoxic Activity of New Vindoline Derivatives Coupled to Natural and Synthetic Pharmacophores |
| title | Synthesis and Cytotoxic Activity of New Vindoline Derivatives Coupled to Natural and Synthetic Pharmacophores |
| title_full | Synthesis and Cytotoxic Activity of New Vindoline Derivatives Coupled to Natural and Synthetic Pharmacophores |
| title_fullStr | Synthesis and Cytotoxic Activity of New Vindoline Derivatives Coupled to Natural and Synthetic Pharmacophores |
| title_full_unstemmed | Synthesis and Cytotoxic Activity of New Vindoline Derivatives Coupled to Natural and Synthetic Pharmacophores |
| title_short | Synthesis and Cytotoxic Activity of New Vindoline Derivatives Coupled to Natural and Synthetic Pharmacophores |
| title_sort | synthesis and cytotoxic activity of new vindoline derivatives coupled to natural and synthetic pharmacophores |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7070384/ https://www.ncbi.nlm.nih.gov/pubmed/32102414 http://dx.doi.org/10.3390/molecules25041010 |
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