N-sübstitüe-3-methylindol türevlerinin sentezi ve biyolojik etkilerinin incelenmesi

In this study, ten novel compounds with the general structure of 1-[(substituted-1-piperidinyl)methyl)]-3-methyl-1H-indole and 1-[(4-(substituted-1-piperazinyl)methyl)]-3-methyl-1H-indole, were synthesized using one-pot reaction method. In order to obtain the desired compounds a mixture of 3-methylindole, formaldehyde and various substituted piperidine and piperazine derivatives were reacted in ethanol under reflux condition for 4-6 hrs. The structure elucidation of the synthesized compounds was confirmed using FT-IR, 1H-NMR and 13C-NMR spectroscopic methods. The antimicrobial activity of the compounds was assessed using the disc diffusion method, the results indicated that compounds 1, 2, ,7 and 10 revealed the highest antibacterial activity against Enterococcus hirae, Enterococcus faecalis, Staphylococcus aureus with inhibition zone of 20 mm, and the highest anti-fungal activity against Candida albicans with inhibition zone of 15 mm. Reference compounds used were ofloxacin for the antibacterial study and nystatin for the antifungal study. In vitro cytotoxic activity screening of the compounds was performed against breast cancer (MCF-7) and noncancerous Human Umbilical Vein Endothelial (HUVEC) cell lines. Compounds 1, 2, 3, 9 and 10 exhibited selective inhibitory effect on MCF-7 cells with an IC50 values of 27, 53, 35, 32 and 31 μM respectively. Tamoxifen was used as a reference drug.