Synthesis, in vitro and in silico studies on novel 3-aryloxymethyl-5-[(2-oxo-2-arylethyl)sulfanyl]-1,2,4-triazoles and their oxime derivatives as potent inhibitors of mPGES-1

Erensoy, Gizem; Ding, Kai; Zhan, Chang‐Guo; Çiftçi, Gamze; Yelekçi, Kemal; Duracik, Merve; Özakpınar, Özlem Bingöl; Aydemir, Esra; Yilmaz, Zübeyde Nur; Şahi̇n, Fikrettin; Kulabaş, Necla; Tatar, Esra; Küçükgüzel, İlkay

doi:10.1016/j.molstruc.2022.134154

Cited by 4 publications

(2 citation statements)

References 78 publications

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“…Expression of mPGES-1 enzyme is increased in the presence of inflammation. The design of selective new mPGES-1 inhibitors as anticancer [21][22][23] and anti-inflammatory [24] agents aiming to block PGE2 production by inhibiting the mPGES-1 enzyme remains up-to-date [25].…”

Section: Introductionmentioning

confidence: 99%

In silico investigation of novel 5-benzylidene-2- (arylsulfonylhydrazono)thiazolidine-4-ones as potential inhibitors of mPGES-1 and COX-2.

KULABAŞ

2023

jrp

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Section: Introductionmentioning

confidence: 99%

In silico investigation of novel 5-benzylidene-2- (arylsulfonylhydrazono)thiazolidine-4-ones as potential inhibitors of mPGES-1 and COX-2.

KULABAŞ

2023

jrp

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“…It exhibits a wide range of biological activities such as anti-tuberculosis (Küçükgüzel, Küçükgüzel, Rollas, & Kiraz, 2001), anti-inflammatory (Küçükgüzel et al, 2007) and anticancer activities (Kulabaş et al, 2016) due to their ability to easily bind to different macromolecular targets with weak interactions. Moreover, many 1,2,4-triazole-thioether derivatives were evaluated as anticancer (Demirbolat et al, 2022;Kulabaş et al, 2016;Zengin, Unsal Tan, Arafa, & Balkan, 2022) agents whereas several reports indicate them as potential inhibitors of mPGES-1 (Bülbül et al, 2022;Erensoy et al, 2023;He, Li, Liu, & Lai, 2013).…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Paracetamol-Triazole Conjugates

KULABAŞ,

GÜRBOĞA,

BİNGÖL ÖZAKPINAR

et al. 2023

Fabad J Pharm Sci

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Some new triazole containing acetamide derivatives 9-20 using paracetamol as starting material were synthesized and their structure were characterized by FTIR, 1H-NMR, 13C-NMR and MS data. In vitro cytotoxic activities of all synthesized molecules against five cancer cell lines (human lung cancer A549, human chronic myelogenous leukemia K562, human breast cancer MCF-7, human prostate cancer PC-3, human neuroblastoma SH-SY5Y cell lines) were examined and were also tested their cytotoxic effect on mouse embryonic fibroblast cells (NIH/3T3) to define selectivity. MTT assay were used these in vitro activity studies. Additionally, twelve target compounds 9-20 were screened for their mPGES-1 and COX-1/2 inhibitory activities. While none of the synthesized compounds showed a significant inhibition against both cancer cells and mPGES-1 as well as COX-1/2, it was determined that they were not cytotoxic against healthy cells, too. Finally, ADMET data were presented by predicting the drug-like properties of newly synthesized compounds using computational methods.

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Recent developments in the chemistry of 1H- and 4H-1,2,4-triazoles

Abbas

Dawood

2023

Advances in Heterocyclic Chemistry

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Synthesis, in vitro and in silico studies on novel 3-aryloxymethyl-5-[(2-oxo-2-arylethyl)sulfanyl]-1,2,4-triazoles and their oxime derivatives as potent inhibitors of mPGES-1

Cited by 4 publications

References 78 publications

In silico investigation of novel 5-benzylidene-2- (arylsulfonylhydrazono)thiazolidine-4-ones as potential inhibitors of mPGES-1 and COX-2.

In silico investigation of novel 5-benzylidene-2- (arylsulfonylhydrazono)thiazolidine-4-ones as potential inhibitors of mPGES-1 and COX-2.

Synthesis and Biological Evaluation of Novel Paracetamol-Triazole Conjugates

Recent developments in the chemistry of 1H- and 4H-1,2,4-triazoles

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