Novel 1,2,4-triazoles derived from Ibuprofen: synthesis and in vitro evaluation of their mPGES-1 inhibitory and antiproliferative activity

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Date

2022

Authors

Ding, Kai
Zhan, Chang-Guo
Ciftci, Gamze
Yelekci, Kemal
Gurboga, Merve
Ozakpinar, Ozlem Bingol

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Springer

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Abstract

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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Keywords

Prostaglandin-E Synthase-1, Antiinflammatory Activity, Hybrids Synthesis, Beta-Catenin, Tumor-Growth, Derivatives, Cox-2, Discovery, Design, Antibacterial, Prostaglandin-E Synthase-1, Antiinflammatory Activity, Hybrids Synthesis, 1,2,4-Triazole, Beta-Catenin, Atropisomer, Tumor-Growth, Diastereotope, Derivatives, X-ray diffraction, Cox-2, Cancer, Discovery, Angiogenesis, Design, mPGES-1, Antibacterial, Cytotoxicity

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4

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N/A

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Q2

Source

Molecular Diversity

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