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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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dc.contributor.authorBİNGÖL ÖZAKPINAR, ÖZLEM
dc.contributor.authorKULABAŞ, NECLA
dc.contributor.authorTATAR, ESRA
dc.contributor.authorKÜÇÜKGÜZEL, İLKAY
dc.contributor.authorsBulbul B., Ding K., Zhan C., Ciftci G., YELEKÇİ K., Gurboga M., BİNGÖL ÖZAKPINAR Ö., Aydemir E., Baybag D., ŞAHİN F., et al.
dc.date.accessioned2022-12-01T08:49:31Z
dc.date.available2022-12-01T08:49:31Z
dc.date.issued2022-11-01
dc.description.abstractSome 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.
dc.identifier.citationBulbul B., Ding K., Zhan C., Ciftci G., YELEKÇİ K., Gurboga M., BİNGÖL ÖZAKPINAR Ö., Aydemir E., Baybag D., ŞAHİN F., et al., "Novel 1,2,4-triazoles derived from Ibuprofen: synthesis and in vitro evaluation of their mPGES-1 inhibitory and antiproliferative activity", MOLECULAR DIVERSITY, 2022
dc.identifier.doi10.1007/s11030-022-10551-0
dc.identifier.issn1381-1991
dc.identifier.urihttps://hdl.handle.net/11424/283407
dc.language.isoeng
dc.relation.ispartofMOLECULAR DIVERSITY
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectTemel Eczacılık Bilimleri
dc.subjectEczacılık
dc.subjectYaşam Bilimleri
dc.subjectMoleküler Biyoloji ve Genetik
dc.subjectSitogenetik
dc.subjectKimya
dc.subjectBiyokimya
dc.subjectAlkoloidler
dc.subjectSağlık Bilimleri
dc.subjectDiğer
dc.subjectTemel Bilimler
dc.subjectBasic Pharmaceutics Sciences
dc.subjectPharmacology and Therapeutics
dc.subjectLife Sciences
dc.subjectMolecular Biology and Genetics
dc.subjectCytogenetic
dc.subjectChemistry
dc.subjectBiochemistry
dc.subjectAlcaloides
dc.subjectHealth Sciences
dc.subjectOther
dc.subjectNatural Sciences
dc.subjectBİYOKİMYA VE MOLEKÜLER BİYOLOJİ
dc.subjectYaşam Bilimleri (LIFE)
dc.subjectKİMYA, UYGULAMALI
dc.subjectTemel Bilimler (SCI)
dc.subjectKİMYA, TIBBİ
dc.subjectKİMYA, MULTİDİSİPLİNER
dc.subjectFARMAKOLOJİ VE ECZACILIK
dc.subjectFarmakoloji ve Toksikoloji
dc.subjectBIOCHEMISTRY & MOLECULAR BIOLOGY
dc.subjectMOLECULAR BIOLOGY & GENETICS
dc.subjectLife Sciences (LIFE)
dc.subjectCHEMISTRY, APPLIED
dc.subjectCHEMISTRY
dc.subjectNatural Sciences (SCI)
dc.subjectCHEMISTRY, MEDICINAL
dc.subjectCHEMISTRY, MULTIDISCIPLINARY
dc.subjectPHARMACOLOGY & PHARMACY
dc.subjectPHARMACOLOGY & TOXICOLOGY
dc.subjectFarmakoloji
dc.subjectİlaç Keşfi
dc.subjectFarmakoloji, Toksikoloji ve Eczacılık (çeşitli)
dc.subjectGenel Farmakoloji, Toksikoloji ve Eczacılık
dc.subjectFarmakoloji (tıbbi)
dc.subjectİlaç Rehberleri
dc.subjectKimya (çeşitli)
dc.subjectGenel Kimya
dc.subjectProses Kimyası ve Teknolojisi
dc.subjectYapısal Biyoloji
dc.subjectMoleküler Biyoloji
dc.subjectKlinik Biyokimya
dc.subjectKanser Araştırmaları
dc.subjectYaşlanma
dc.subjectBiyokimya, Genetik ve Moleküler Biyoloji (çeşitli)
dc.subjectGenel Biyokimya, Genetik ve Moleküler Biyoloji
dc.subjectFizik Bilimleri
dc.subjectPharmacy
dc.subjectPharmacology
dc.subjectDrug Discovery
dc.subjectPharmacology, Toxicology and Pharmaceutics (miscellaneous)
dc.subjectGeneral Pharmacology, Toxicology and Pharmaceutics
dc.subjectPharmacology (medical)
dc.subjectDrug Guides
dc.subjectChemistry (miscellaneous)
dc.subjectGeneral Chemistry
dc.subjectProcess Chemistry and Technology
dc.subjectStructural Biology
dc.subjectMolecular Biology
dc.subjectClinical Biochemistry
dc.subjectCancer Research
dc.subjectAging
dc.subjectBiochemistry, Genetics and Molecular Biology (miscellaneous)
dc.subjectGeneral Biochemistry, Genetics and Molecular Biology
dc.subjectPhysical Sciences
dc.subject1,2,4-Triazole
dc.subjectAtropisomer
dc.subjectDiastereotope
dc.subjectX-ray diffraction
dc.subjectCancer
dc.subjectAngiogenesis
dc.subjectmPGES-1
dc.subjectCytotoxicity
dc.subjectPROSTAGLANDIN-E SYNTHASE-1
dc.subjectANTIINFLAMMATORY ACTIVITY
dc.subjectHYBRIDS SYNTHESIS
dc.subjectBETA-CATENIN
dc.subjectTUMOR-GROWTH
dc.subjectDERIVATIVES
dc.subjectCOX-2
dc.subjectDISCOVERY
dc.subjectDESIGN
dc.subjectANTIBACTERIAL
dc.titleNovel 1,2,4-triazoles derived from Ibuprofen: synthesis and in vitro evaluation of their mPGES-1 inhibitory and antiproliferative activity
dc.typearticle
dspace.entity.typePublication
local.avesis.idf8bed34f-45a1-4561-931b-49a142ef7954
local.indexed.atWOS
local.indexed.atPUBMED
local.indexed.atSCOPUS
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relation.isAuthorOfPublication39266c2c-11fd-48a6-8455-d3ea2f2956ed
relation.isAuthorOfPublication.latestForDiscovery44b61e5d-4045-4d63-926e-2f01c3ee5642

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