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

This paper presents the synthesis of [Formula: see text]-halo- [Formula: see text]-lactones, [Formula: see text]-iodo- [Formula: see text]-lactones and [Formula: see text]-hydroxy- [Formula: see text]-lactones from readily available organic substrates such as trans-crotonaldehyde and aryl bromides....

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Detalles Bibliográficos
Autores principales: Kamizela, Angelika, Gawdzik, Barbara, Urbaniak, Mariusz, Lechowicz, Łukasz, Białońska, Agata, Kutniewska, Sylwia Ewa, Gonciarz, Weronika, Chmiela, Magdalena
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6572184/
https://www.ncbi.nlm.nih.gov/pubmed/31096674
http://dx.doi.org/10.3390/molecules24101875
Descripción
Sumario:This paper presents the synthesis of [Formula: see text]-halo- [Formula: see text]-lactones, [Formula: see text]-iodo- [Formula: see text]-lactones and [Formula: see text]-hydroxy- [Formula: see text]-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- [Formula: see text]-lactones and [Formula: see text]-hydroxy- [Formula: see text]-lactones were highly cytotoxic against gastric cancer AGS cells with [Formula: see text] 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.