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Research Article

Synthesis and bioactivity studies of 1-aryl-3-(2-hydroxyethylthio)-1-propanones

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Pages 105-109 | Received 07 Jun 2016, Accepted 30 Jun 2016, Published online: 19 Jul 2016
 

Abstract

A series of Mannich bases having piperidine moiety were reacted with 2-mercaptoethanol, leading to 1-aryl-3-piperidine-4-yl-1-propanone hydrochlorides. The cytotoxicity and carbonic anhydrase inhibitory activities of these new compounds were evaluated. Among the compounds, only one derivative, nitro substituent bearing EU9, showed an effective cytotoxicity, although weak tumor specificity against human oral malignant versus nonmalignant cells. The compound induced apoptosis in HSC-2 oral squamous cell carcinoma cells, but not in human gingival fibroblast. Chemical modifications of this lead are thus necessary to further investigate it as a drug candidate and to obtain compounds with a better activity profile.

Acknowledgements

Professor Gul HI thanks Dr. Murat Sukuroglu from Gazi University for HRMS.

Declaration of interest

This study was supported by Ataturk University (BAP Project Number: 2010/166). The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.

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