Molecules, Vol. 25, Pages 888: Synthesis and In Vitro Anticancer Evaluation of Novel Chrysin and 7-Aminochrysin Derivatives
Molecules, Vol. 25, Pages 888: Synthesis and In Vitro Anticancer Evaluation of Novel Chrysin and 7-Aminochrysin Derivatives
Molecules doi: 10.3390/molecules25040888
Authors:
Mayer
Keglevich
Ábrányi-Balogh
Szigetvári
Dékány
Szántay
Hazai
Chrysin is a naturally occurring flavonoid with mild anticancer activity. In this paper we report the synthesis of new chrysin derivatives alkylated with N-phenylchloroacetamides in position 7. A novel method was developed for the preparation of 7-aminochrysin derivatives via the Smiles rearrangement, resulting in diphenylamine-type compounds. In silico studies of the Smiles rearrangement were performed. We also present the in vitro antiproliferative activity of the synthesized compounds against 60 human tumor cell lines (NCI60). The most potent derivative exhibited nanomolar antitumor activity on the MCF7 cell line of breast cancer (GI50 = 30 nM) and on the HCT-15 cell line of colon cancer (GI50 = 60 nM).
Source: Molecules - Category: Chemistry Authors: Mayer Keglevich Ábrányi-Balogh Szigetv ári D ékány Sz ántay Hazai Tags: Article Source Type: research
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