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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

General Research Article

Novel Tri-substituted Thiazoles Bearing Piperazine Ring: Synthesis and Evaluation of their Anticancer Activity

Author(s): Asaf Evrim Evren*, Leyla Yurttaş, Busra Eksellı and Gulsen Akalın-Cıftcı

Volume 16, Issue 5, 2019

Page: [547 - 555] Pages: 9

DOI: 10.2174/1570180815666180731122118

Price: $65

Abstract

Background: Cancer cells are described as an unregulated growth and spread of abnormal cells. Recently, cancer has become the most important major reason for deaths in the world.

Methods: For anticancer activity, we have used the MTT method and determine the early/late apoptosis by flow cytometry.

Results: The title compounds were procured by reacting 2-chloro-N-[4-(pyridin-4-yl)thiazol-2- yl]acetamide with some substituted piperazine derivatives. The in vitro anticancer activity of synthesized compounds was tested against C6 rat glioma cells and A549 human lung carcinoma cells. As a result, the compounds 3d, 3e, 3f and 3g have shown anticancer activity against both cell line.

Conclusion: Specifically, compound 3f was determined as the most active compound against C6 rat glioma cells. Also, as understood, the core structure which is substituted with piperazine bridge, the heterocyclic aromatic derivatives are more active than phenyl or benzyl derivatives.

Keywords: Thiazole, azole, piperazine, acetamide, anticancer activity, phenyl, benzyl.

Graphical Abstract
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