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.
Highlights
The famous Vinca alkaloid family was isolated first in the 1950s from the leaves of Catharanthus roseus
A significant antitumor effect was presumed by connecting amino acids [(l)- or (d)-tryptophan]
10-aminovindoline (5) and 17-desacetylvindoline (9) with the aforementioned scaffolds resulted in new Vinca alkaloid derivatives. a few of these compounds (11, 12, and 24) demonstrated promising antitumor effect, and may be considered as promising leads, against certain types of cervical cancer
Summary
The famous Vinca alkaloid family was isolated first in the 1950s from the leaves of Catharanthus roseus. Some of these natural compounds, along with their semisynthetic analogues, are still being used as chemotherapeutic agents in anticancer therapy (especially in the case of lymphomas and leukemia) [1,2,3,4,5,6,7,8,9,10,11,12,13,14,15]. Vindoline (1) is present in the plant in a much larger quantity than the dimers, it does not have any anticancer effect. We have attempted to test vindoline (1) as a potential antitumor agent by connecting it to different natural and synthetic pharmacophores
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