New γ-Halo- δ-lactones and δ-Hydroxy- γ-lactones with Strong Cytotoxic Activity

具有强细胞毒活性的新型 γ-卤代-δ-内酯和δ-羟基-γ-内酯

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作者:Angelika Kamizela, Barbara Gawdzik, Mariusz Urbaniak, Łukasz Lechowicz, Agata Białońska, Sylwia Ewa Kutniewska, Weronika Gonciarz, Magdalena Chmiela

Abstract

This paper presents the synthesis of γ -halo- δ -lactones, δ -iodo- γ -lactones and δ -hydroxy- γ -lactones from readily available organic substrates such as trans-crotonaldehyde and aryl bromides. Crystal structure analysis was carried out for lactones that were obtained in crystalline form. All halo- δ -lactones and δ -hydroxy- γ -lactones were highly cytotoxic against gastric cancer AGS cells with I C 50 values in the range of 0.0006-0.0044 mM. Some lactones showed high bactericidal activity against E. coli ATCC 8739 and S. aureus ATCC 65389, which reduced the number of CFU/mL by 70-83% and 87% respectively.

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