New Thiazoline-Tetralin Derivatives and Biological Activity Evaluation

• Published in: Molecules (Basel, Switzerland) Switzerland), 2018-01, Vol.23 (1), p.135
• Main Authors: Turan-Zitouni, Gülhan, Yurttaş, Leyla, Tabbi, Aouatef, Akalın Çiftçi, Gülşen, Temel, Halide Edip, Kaplancıklı, Zafer Asım
• Format: Article
• Language: English
• Subjects: A549 Cells; Acetylcholinesterase; Adenocarcinoma; Animals; Antibiotics; anticholinesterase activity; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Apoptosis; Biological activity; Bladder; Cancer; Cell division; Cell Survival; Cholinesterase Inhibitors - chemistry; Cholinesterase Inhibitors - pharmacology; Cisplatin; Cisplatin - chemistry; Cisplatin - pharmacology; Clinical trials; Cytotoxicity; Dementia; Deoxyribonucleic acid; DNA; DNA biosynthesis; DNA synthesis inhibition; Drug resistance; Drug Screening Assays, Antitumor - methods; Enzymes; Flow cytometry; Glaucoma; Humans; Hydrazines - chemistry; Hydrazines - pharmacology; Inhibition; Lung carcinoma; Magnetic Resonance Spectroscopy - methods; Mass Spectrometry - methods; MCF-7 Cells; Mice; Molecular Structure; Myasthenia gravis; NIH 3T3 Cells; Nucleic Acid Synthesis Inhibitors - chemistry; Nucleic Acid Synthesis Inhibitors - pharmacology; Parkinson's disease; Pharmacy; Structure-Activity Relationship; Tetralin; tetralin (tetrahydronaftalene); Thiazoline; Triazoles - chemistry; Triazoles - pharmacology
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules23010135

In this study, novel '-(3-cyclohexyl/phenyl-4-(substituted phenyl)thiazole-2(3 )-ylidene)-2-[(5,6,7,8-tetrahydronaphthalen-2-yl)oxy]acetohydrazide ( - ) 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 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 , , and 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 showed 49.92% inhibition of acetylcholinesterase (AChE).