Synthesis and biological activities of dithiocarbamates containing 2(5H)-furanone-piperazine

A series of new dithiocarbamates containing a 2(5H)-furanone-piperazine group was synthesized. These compounds show good in vitro cytoxic activity. Among them, compound 6c exhibits the best inhibitory activity against HeLa cell lines with an IC50 of 0.06 ± 0.01 μM for 72 h, and it has good inhibitor...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:European journal of medicinal chemistry 2018-07, Vol.155, p.165-170
Hauptverfasser: Wei, Meng-Xue, Zhang, Jiao, Ma, Fu-Li, Li, Ming, Yu, Jia-Ying, Luo, Wei, Li, Xue-Qiang
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:A series of new dithiocarbamates containing a 2(5H)-furanone-piperazine group was synthesized. These compounds show good in vitro cytoxic activity. Among them, compound 6c exhibits the best inhibitory activity against HeLa cell lines with an IC50 of 0.06 ± 0.01 μM for 72 h, and it has good inhibitory activity against SMMC-7721 cell lines with an IC50 of 0.006 ± 0.04 μM for 72 h, but the toxicity was lower against LO2 cell lines with an IC50 of 45.76 ± 0.01 μM. The result showed that compound 6c is far more cytoxic towards cancer cell lines than towards benign cell lines compared with cytosine arabinoside (ARA) in vitro. [Display omitted] •The dithiocarbamates containing a 2(5H)-furanone-piperazine were synthesized.•The target compounds showed good cytoxic activity.•Compound 6c is far more cytoxic against cancer cells than against benign cells.•Compound 6b has higher cytoxic activity against SMMC-7721 cell lines than ARA.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2018.05.056