Antiproliferative activity of some tautomeric hydrazones derived from chalcones


Creative Commons License

TOK F., Beyhan N., ERZURUMLU Y., İLHAN R. , Ballar P. , Kocyigit-Kaymakcioglu B.

MARMARA PHARMACEUTICAL JOURNAL, cilt.20, ss.157-163, 2016 (ESCI İndekslerine Giren Dergi) identifier identifier

  • Cilt numarası: 20 Konu: 2
  • Basım Tarihi: 2016
  • Doi Numarası: 10.12991/mpj.20162093956
  • Dergi Adı: MARMARA PHARMACEUTICAL JOURNAL
  • Sayfa Sayıları: ss.157-163

Özet

A new series of hydrazones synthesized from chalcones. Synthesized compounds have been characterized by IR, H-1-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 mu M. 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.