Antiproliferative activity of some tautomeric hydrazones derived from chalcones
| Autor: | Recep Ilhan, Petek Ballar, Fatih Tok, Bedia Kaymakçioğlu, Yalcin Erzurumlu, Nagihan Beyhan |
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| Přispěvatelé: | Tok, Fatih, Beyhan, Nagihan, Erzurumlu, Yalcin, Ilhan, Recep, Ballar, Petek, Kocyigit-Kaymakcioglu, Bedia |
| Jazyk: | angličtina |
| Rok vydání: | 2015 |
| Předmět: |
antiproliferative activity
biology chalcones DERIVATIVES 010405 organic chemistry Stereochemistry Chemistry 010402 general chemistry biology.organism_classification Reference drug 01 natural sciences Tautomer 0104 chemical sciences HeLa Cell culture hydraxones medicine Pharmacology (medical) Doxorubicin POTENTIAL ANTICANCER AGENTS General Pharmacology Toxicology and Pharmaceutics Cytotoxicity medicine.drug |
| Popis: | A new series of hydrazones synthesized from chalcones. Synthesized compounds have been characterized by IR, 1 H-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 IC 50 =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 IC 50 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 IC 50 concentration. None of the tested compounds changed the level of total polyubiquitinated proteins. Keywords: chalcones, hydrazones, antiproliferative activity |
| Databáze: | OpenAIRE |
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