Inhibitor and Apoptotic Anticancer Agents

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 mu M for CaCo-2, 29 mu M for LnCaP, 14 mu M for MDA-MB231, 21 mu M for HepG2 and 87 mu M 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.C1 [Konus, Metin; Cetin, Dogan; Yilmaz, Can; Ozok, Omruye] Van Yuzuncu Yil Univ, Dept Mol Biol & Genet, Fac Sci, TR-65080 Van, Turkey.[Arslan, Sevki; Mutlu, Dogukan] Pamukkale Univ, Dept Biol, Fac Arts & Sci, TR-20100 Denizli, Turkey.[Kurt-Kizildogan, Aslihan; Otur, Cigdem] Ondokuz Mayis Univ, Dept Agr Biotechnol, Fac Agr, TR-55139 Samsun, Turkey.[Ozok, Omruye; Algso, Muheb A. S.; Kivrak, Arif] Van Yuzuncu Yil Univ, Dept Chem, TR-65080 Van, Turkey