New Thiazoline-Tetralin Derivatives and Biological Activity Evaluation

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Turan-Zitouni G., YURTTAŞ L., Tabbi A., AKALIN ÇİFTÇİ G., TEMEL H. E., KAPLANCIKLI Z. A.

MOLECULES, cilt.23, sa.1, 2018 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 23 Sayı: 1
  • Basım Tarihi: 2018
  • Doi Numarası: 10.3390/molecules23010135
  • Dergi Adı: MOLECULES
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Anahtar Kelimeler: thiazoline, tetralin (tetrahydronaftalene), cytotoxicity, DNA synthesis inhibition, apoptosis, anticholinesterase activity, ANTICANCER ACTIVITY, 5,6,7,8-TETRAHYDRONAPHTHALENE DERIVATIVES, ANTIOXIDANT ACTIVITY, AGENTS, ANTITUMOR, INHIBITORS, CANCER, APOPTOSIS, POTENT, CELLS
  • Anadolu Üniversitesi Adresli: Evet

Özet

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 (4a-4k) 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).