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TATAR, ESRA

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TATAR

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ESRA

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2013 - 201912020 - 20222
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    PublicationOpen Access
    Novel 1,2,4-triazoles derived from Ibuprofen: synthesis and in vitro evaluation of their mPGES-1 inhibitory and antiproliferative activity
    (2022-11-01) BİNGÖL ÖZAKPINAR, ÖZLEM; KULABAŞ, NECLA; TATAR, ESRA; KÜÇÜKGÜZEL, İLKAY; Bulbul B., Ding K., Zhan C., Ciftci G., YELEKÇİ K., Gurboga M., BİNGÖL ÖZAKPINAR Ö., Aydemir E., Baybag D., ŞAHİN F., et al.
    Some novel triazole-bearing ketone and oxime derivatives were synthesized from Ibuprofen. In vitro cytotoxic activities of all synthesized molecules against five cancer lines (human breast cancer MCF-7, human lung cancer A549, human prostate cancer PC-3, human cervix cancer HeLa, and human chronic myelogenous leukemia K562 cell lines) were evaluated by MTT assay. In addition, mouse embryonic fibroblast cells (NIH/3T3) were also evaluated to determine the selectivity. Compounds 18, 36, and 45 were found to be the most cytotoxic, and their IC50 values were in the range of 17.46-68.76 mu M, against the tested cancer cells. According to the results, compounds 7 and 13 demonstrated good anti-inflammatory activity against the microsomal enzyme prostaglandin E2 synthase-1 (mPGES-1) enzyme at IC50 values of 13.6 and 4.95 mu M. The low cytotoxicity and non-mutagenity of these compounds were found interesting. Also, these compounds significantly prevented tube formation in angiogenesis studies. In conclusion, the anti-inflammatory and angiogenesis inhibitory activities of these compounds without toxicity suggested that they may be promising agents in anti-inflammatory treatment and they may be supportive agents for the cancer treatment.
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    PublicationOpen Access
    2-Heteroarylimino-5-arylidene-4-thiazolidinones as a new class of non-nucleoside inhibitors of HCV NS5B polymerase
    (ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 2013-11) TATAR, ESRA; Kucukguzel, Ilkay; Satilmis, Gokhan; Gurukumar, K. R.; Basu, Amartya; Tatar, Esra; Nichols, Daniel B.; Talele, Tanaji T.; Kaushik-Basu, Neerja
    Hepatitis C virus (HCV) NS5B polymerase is an important and attractive target for the development of anti-HCV drugs. Here we report on the design, synthesis and evaluation of twenty-four novel allosteric inhibitors bearing the 4-thiazolidinone scaffold as inhibitors of HCV NS5B polymerase. Eleven compounds tested were found to inhibit HCV NS5B with IC50 values ranging between 19.8 and 64.9 RM. Compound 24 was the most active of this series with an IC50 of 5.6 mu M. A number of these derivatives further exhibited strong inhibition against HCV lb and 2a genotypes in cell based antiviral assays. Molecular docking analysis predicted that the thiazolidinone derivatives bind to the NS5B thumb pocketII (TP-II). Our results suggest that further optimization of the thiazolidinone scaffold may be possible to yield new derivatives with improved enzyme- and cell-based activity. (C) 2013 Elsevier Masson SAS. All rights reserved.
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    PublicationOpen Access
    Synthesis, characterization and biological evaluation of 1,3-thiazolidine-4-ones derived from (2S)-2-benzoylamino-3-methylbutanohydrazide hydrazones
    (MARMARA UNIV, 2021) TATAR, ESRA; Tatar, Esra; Kucukguzel, Ilkay; Otuk, Gulten; Bilgin, Merve; De Clercq, Erik; Andrei, Graciela; Snoeck, Robert; Pannecouque, Christophe; Kaushik-Basu, Neerja
    Novel 2-aryl-5-non-substituted / methyl-1,3-thiazolidine-4-one derivatives 14-33 carrying L-valine core were synthesized by the reaction of acylhydrazones 4-13 with thioglycolic acid / thiolactic acid. Structures of all synthesized compounds 14-33 were confirmed by IR, H-1-NMR and HR-MS analysis and C-13-NMR were recorded for selected compounds 17, 21, 28 and 30. None of the compounds 14-33 showed activity against HIV-1 (strain IIIB) or HIV-2 (strain ROD) in an MT-4/MTT based assay. Compounds 14-33 were also screened against Feline Corona Virus (FIPV), Feline Herpes Virus, HSV-1(KOS), HSV-1 (TK-KOS ACVr), HSV-2 (G), Vaccinia virus, Vesicular stomatitis virus, Cytomegalovirus, Varicella-Zoster virus, Respiratory syncytial virus, Coxsackie B4 virus, Parainfluenza-3 virus, Reovirus-1, Sindbis virus and Punta Toro virus, but none of them showed antiviral activity at subtoxic concentrations. Anti-HCV NS5B RdRp activity of some selected compounds from the series 14-33 were found to vary between 4.1-27 % at the concentration of 100 mu M. In vitro antibacterial activity evaluation of selected compounds 16-23 and 25-32, against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Enterococcus faecalis ATCC 29212, Klebsiella pneumoniae ATCC 4352, Bacillus subtilis ATCC 6633, Staphylococcus epidermidis ATCC 12228, MRSA and antifungal activity against Candida albicans ATCC 10231 resulted in the MIC values between 625->5000 mu g/ml.