Synthesis of Novel Vindoline‐Chrysin Hybrids

Autor: Szabolcs Mayer, Nóra Nagy, Péter Keglevich, Áron Szigetvári, Miklós Dékány, Csaba Szántay Junior, László Hazai
Rok vydání: 2021
Předmět:
Zdroj: Chemistry & Biodiversity. 19
ISSN: 1612-1880
1612-1872
Popis: Vinca alkaloids are well-known microtubule targeting agents, which are used against some types of cancer. Vindoline is one of the monomeric Vinca alkaloids which does not have anti-tumor effect, although its derivatives have serious impact on the field of these indole alkaloids. Chrysin is a secondary plant metabolite, which has broad-spectrum biological activity, among others anticancer activity. Chrysin had shown synergic effect with several antiproliferative compounds (e. g., doxorubicin, cisplatin and ciglitazone), therefore, we attempted the synthesis of a novel vindoline-chrysin hybrid molecule. However, in the first case a diphenylamine structure was isolated. The mechanism of the unexpected reaction was studied, and then the originally targeted hybrid was synthesized by a reverse route coupling. A further hybrid was produced using a different site of the molecule. The antitumor activities were determined against 60 human tumor cell lines (NCI60), where the aimed hybrid showed low micromolar GI
Databáze: OpenAIRE
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