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Molecules 2018, 23(1), 135; https://doi.org/10.3390/molecules23010135

New Thiazoline-Tetralin Derivatives and Biological Activity Evaluation

1
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskisehir, Turkey
2
Department of Chemistry, Faculty of Sciences, Mentouri University, 25000 Constantin, Algeria
3
Department of Biochemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskisehir, Turkey
*
Author to whom correspondence should be addressed.
Received: 27 December 2017 / Revised: 7 January 2018 / Accepted: 9 January 2018 / Published: 10 January 2018
(This article belongs to the Section Medicinal Chemistry)
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Abstract

In this study, novel N′-(3-cyclohexyl/phenyl-4-(substituted phenyl)thiazole-2(3H)-ylidene)-2-[(5,6,7,8-tetrahydronaphthalen-2-yl)oxy]acetohydrazide (4a4k) derivatives were synthesized and their anticancer potency were evaluated on human breast adenocarcinoma cell line (MCF-7), human lung carcinoma cell line (A549) and mouse embryoblast cell line (NIH/3T3) using the MTT method, DNA synthesis inhibition and flow cytometric analysis. Compound 4e bearing 4-methoxyphenyl moiety exhibited the highest antitumor efficiency against MCF-7 cell line with higher DNA synthesis inhibition and apoptotic cell percentages (ealy+late apoptotic cell). On the other hand, compounds 4f, 4g, and 4h bearing 4-bromo, 4-chloro and 4-florophenyl moieties, respectively caused excellent apoptosis levels against A549 cell line when treated with lower concentration even than cisplatin. Anticholinesterase activity of the compounds were also tested, compound 4h showed 49.92% inhibition of acetylcholinesterase (AChE). View Full-Text
Keywords: thiazoline; tetralin (tetrahydronaftalene); cytotoxicity; DNA synthesis inhibition; apoptosis; anticholinesterase activity thiazoline; tetralin (tetrahydronaftalene); cytotoxicity; DNA synthesis inhibition; apoptosis; anticholinesterase activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Turan-Zitouni, G.; Yurttaş, L.; Tabbi, A.; Akalın Çiftçi, G.; Temel, H.E.; Kaplancıklı, Z.A. New Thiazoline-Tetralin Derivatives and Biological Activity Evaluation. Molecules 2018, 23, 135.

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