Çiftçi, Gamze

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Çiftçi, Gamze
G.,Çiftçi
G. Çiftçi
Gamze, Çiftçi
Ciftci, Gamze
G.,Ciftci
G. Ciftci
Gamze, Ciftci
Job Title
Misafir Öğr. Gör.
Email Address
Gamze.cıftcı@khas.edu.tr
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Scholarly Output

3

Articles

2

Citation Count

0

Supervised Theses

1

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2021 - 20233
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Now showing 1 - 3 of 3
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    Article
    Citation Count: 4
    Novel 1,2,4-Triazoles Derived From Ibuprofen: Synthesis and in Vitro Evaluation of Their Mpges-1 Inhibitory and Antiproliferative Activity
    (Springer, 2022) Bulbul, Bahadir; Ding, Kai; Zhan, Chang-Guo; Ciftci, Gamze; Yelekci, Kemal; Gurboga, Merve; Ozakpinar, Ozlem Bingol
    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. [GRAPHICS] .
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    Article
    Citation Count: 3
    Synthesis, in Vitro and in Silico Studies on Novel 3-Aryloxymethyl and Their Oxime Derivatives as Potent Inhibitors of Mpges-1
    (Elsevier, 2023) Erensoy, Gizem; Ding, Kai; Zhan, Chang-Guo; Ciftci, Gamze; Yelekci, Kemal; Duracik, Merve; Ozakpinar, Ozlem Bingol
    Human microsomal prostaglandin E synthase (mPGES)-1 is a glutathione-dependent membrane-bound enzyme which is involved in the terminal stage of prostaglandin E2 (PGE2) synthesis. It has been well reported as a key target for the discovery of new anti-inflammatory and anti-cancer drugs. Specific in-hibitors of mPGES-1 are anticipated to selectively restrain the generation of PGE2 induced by the in-flammatory stimuli, without obstructing of the regular biosynthesis of other homeostatic prostanoids. Therefore, the design of mPGES-1 inhibitors can represent a better choice to take control of PGE2 asso-ciated diseases, compared with conventional non-steroidal anti-inflammatory drugs and cyclooxygenase (COX) inhibitors, which are known for their serious side effects. Although there is an intensive effort for the identification of mPGES-1 inhibitors, none of the unveiled molecules so far have reached the clini-cal market. Therefore, the development of novel mPGES-1 inhibitors with proper drug-like properties is still an unmet medical need. As a continuation of our research for the identification of new chemotypes which might inhibit this enzyme, we now report the design and synthesis of 3-aryloxymethyl-5-[(2-oxo-2-arylethyl)sulfanyl]-1,2,4-triazoles and their oxime derivatives as inhibitors of human mPGES-1. All syn-thesized compounds were characterized by FTIR, 1 H NMR, 13 C NMR (for compounds 12, 14, 15, 26, 27) , HMBC (for compounds 6, 7, 8, 16, 19, 23, 28), and MS data. Twenty-four target compounds 7-30 were screened for their mPGES-1/COX-2 inhibitory activities as well as their cytotoxicity. Of these compounds, 20 and 24 showed potent mPGES-1 inhibition by IC50 values of 0.224 +/- 0.070 mu M and 1.08 +/- 0.35 mu M, re-spectively. These two compounds have also been observed to inhibit angiogenesis in matrigel tube forma-tion assay with no toxicity toward HUVEC cells. In silico studies were also held to understand inhibition mechanisms of the most active compounds using molecular docking, molecular dynamics calculations and ADMET predictions.(c) 2022 Elsevier B.V. All rights reserved.
  • Thumbnail Image
    Master Thesis
    Design of Novel and Potent Inhibitors for Mpges-1 Enzyme Via in Silico Screening
    (Kadir Has Üniversitesi, 2021) Çiftçi, Gamze; Yelekçi, Kemal
    To prevent inflammation in the body, non-steroidal anti-inflammatory drugs act by suppressing PGE2 production as a result of non-selective inhibition of both COX-1 and COX-2 enzymes. As a result of the inhibition of COX-1 and COX-2, gastrointestinal poisoning and cardiovascular complications occurred, respectively. mPGES-1 inhibitors have been shown to have no known side effects. Thus, inhibition of PGE2 biosynthesis by inhibition of mPGES-1 has become a new therapeutic target in the treatment of inflammatory diseases, which is considered to be clinically safer. In this thesis, approximately 2.5 million ligands were downloaded from the ZINC particle library to screen the mPGES-1 enzyme. Prescreening of these ligands was performed with Autodock-Vina. 1261 compounds were scanned using Autodock 4. Binding energies and poses were determined. Based on the known inhibitor study available on the market. The best inhibitors were subjected to the ADMET test, and molecular dynamic simulation was performed for the four inhibitors determined as the best according to this test, and RMSD, RMSF, and Rg values ​​were analyzed.