Please use this identifier to cite or link to this item: https://hdl.handle.net/11499/37156
Title: Synthesis, Biological Evaluation and Molecular Docking of Novel Thiophene-Based Indole Derivatives as Potential Antibacterial, GST Inhibitor and Apoptotic Anticancer Agents
Authors: Konus, M.
Çetin, D.
Yılmaz, C.
Arslan, Şevki
Mutlu, Doğukan
Kurt-Kızıldoğan, A.
Otur, Ç.
Keywords: antibacterial
apoptotic anticancer agent
cytotoxicity
GST inhibitor
indole
thiophene
Publisher: Wiley-Blackwell
Abstract: Heteroaromatic indoles play a leading role in the development of pharmaceutical, medical, chemical and agricultural fields due to their structural properties. In this study, it was first time that biological properties of (antioxidant, antimicrobial, cytotoxic and apoptotis-induced anticancer) 3-(5-bromothiophen-2-yl)-1-ethyl-2-phenyl-1H-indole 4 and 3-([2,2'-bithiophen]-5-yl)-1-ethyl-2-phenyl-1H-indole 5 were described. According to the overall results, while 4 did not show any significant cytotoxic, antioxidant and antimicrobial activities, 5 showed high reducing activity and very strong antibacterial activity against Enterococcus faecalis. Furthermore, 5 showed dose-dependent cytotoxic effect in all tested cell lines. The EC50 values of the 5 were found to be 16 µM for CaCo-2, 29 µM for LnCaP, 14 µM for MDA-MB231, 21 µM for HepG2 and 87 µM for HEK293 cells, respectively. 5 also caused induction of apoptosis and promising glutathione S-transferase (GST) enzyme inhibition in HepG2 cells. Consequently, 5 could be also considered as a promising medical agent in cancer treatment. © 2020 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
URI: https://hdl.handle.net/11499/37156
https://doi.org/10.1002/slct.202001523
ISSN: 2365-6549
Appears in Collections:Fen-Edebiyat Fakültesi Koleksiyonu
Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection
WoS İndeksli Yayınlar Koleksiyonu / WoS Indexed Publications Collection

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