WoS İndeksli Yayınlar Koleksiyonu

Permanent URI for this collectionhttps://hdl.handle.net/20.500.14627/6

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  • Article
    Citation - Scopus: 1
    Synthesis and Biological Evaluation of New 4-Thiazolidinone Derivatives of Flurbiprofen
    (Acg Publications, 2023) Suzgun, Pelin; Senkardes, Sevil; Gurboga, Merve; Ozakpinar, Ozlem Bingol; Kucukguzel, S. Guniz
    In this study, the synthesis and characterization of 2-(2-fluorobiphenyl-4-yl)-N '-[(substituted methylene]propanehydrazides (3a-s) and 2-(2-fluoro-[1,1'-biphenyl]-4-yl)-N-(5-methyl-2-(substituted aryl)-4oxothiazolidin-3-yl)propanamides (4a-s) are described and also the antiproliferative effect of the compounds on HT 29, HeLa, A549 and MCF-7 cancer cell lines is investigated. Additionally, mouse embryonic fibroblast cells NIH3T3 were also evaluated to determine the selectivity. The results showed that the identified compounds did not cause any toxicity against NIH3T3 cell line. Moreover, N-(2-(3,5-Bis(trifluoromethyl)phenyl)-5-methyl-4-oxothiazolidin-3-yl)-2-(2-fluoro-[1,1'-biphenyl]-4-yl)propanamide (4h) had the most growth inhibitory effect (55.97% inhibition) on HT-29 colorectal adenocarcinoma cell line. The results obtained from the study show that the compound 4h, which has no cytotoxic effect on normal cells, may be an alternative in the treatment of colon cancer.
  • Article
    Citation - WoS: 11
    Citation - Scopus: 11
    Synthesis and Biological Evaluation of Novel Aryloxyacetic Acid Hydrazide Derivatives as Anticancer Agents
    (Taylor & Francis inc, 2021) Senkardes, Sevil; Erdogan, Omer; Cevik, Ozge; Kucukguzel, S. Guniz
    In our continuing search for new anticancer agents, herein we report the synthesis of 2-(4-chloro-3-methylphenoxy)-N'-[(aryl)methylidene]acetohydrazides 3a-j and the evaluation of their anticancer activities on cell viability, morphological changes and caspase-3 activity in cancer cell lines including gastric cancer (MKN45), cervical cancer (HeLa) and breast cancer (MDA-MB-231) cells. 2-(4-chloro-3-methylphenoxy)-N'-[(4-phenylthiophen-2-yl)methylidene] acetohydrazide 3g presented the strongest growth inhibition against MKN45 gastric cancer cell lines with the IC50 value of 1.471 +/- 0.23 mu M. Moreover, compounds 3b and 3g showed high potency against the HeLa and MDA-MB-231 cell lines having IC50 in the range of 2.38-9.72 mu M. These compounds are more selective for the tested human cancer cells than for the mouse fibroblast cell line (NIH/3T3). As a result of the studies conducted in order to understand the molecular mechanism, compounds 3b and 3g enhanced expression of the caspase-3 pro-apoptotic proteins levels besides caspase-3 gene.