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

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.

SUBMITTER: Keglevich A

PROVIDER: S-EPMC7070384 | biostudies-literature | 2020 Feb

REPOSITORIES: biostudies-literature

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

Keglevich András A Dányi Leonetta L Rieder Alexandra A Horváth Dorottya D Szigetvári Áron Á Dékány Miklós M Szántay Csaba C Latif Ahmed Dhahir AD Hunyadi Attila A Zupkó István I Keglevich Péter P Hazai László L

Molecules (Basel, Switzerland) 20200224 4

New <i>Vinca</i> 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 gynecologi ...[more]

PMID: 32102414

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