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...

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Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Article
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
Descripción
Sumario: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.

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