Fatih Tok, Nagihan BeyhaN, Bedia kocyigiT-kaymakcioglu

Year 2016, Volume: 20 Issue: 2, 157 - 163, 10.03.2016

Fatih Tok Nagihan Beyhan Yalçın Erzurumlu Recep İlhan Petek Ballar Bedia Koçyiğit Kaymakçıoğlu

Abstract

Antiproliferative activity of some tautomeric hydrazones derived from chalcones

Abstract

A new series of hydrazones synthesized from chalcones. Synthesized compounds have been characterized by IR, ¹H-NMR and elemental analysis. Antiproliferative activity of compounds was investigated on Hela, A549, MCF7, HCC1937, MRC5 cells. All compounds exhibited cytotoxicity. Especially compounds 1b, 1c, 1f and 1i having 4-metylsulfonyl phenyl showed higher cytotoxicity against all of the cell lines compared to reference drug doxorubicin with low value of IC₅₀=5,56-21,93 µM. The most active compounds 1b, 1c, 1f and 1i were analyzed for their effect on autophagic processes. HCC1937 cells were treated with these compounds at IC₅₀ concentration for 24 hours. An immunoblotting assay was performed to analysis autophagy markers and total polyubiquitinated protein levels. Compounds 1b, 1c, 1f and 1i significantly increased the conversion of LC3-I to LC3-II at IC₅₀ concentration. None of the tested compounds changed the level of total polyubiquitinated proteins.

Keywords: chalcones, hydrazones, antiproliferative activity

Keywords

chalcones, hydrazones, antiproliferative activity