Publication: 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
2022-11-01
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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.
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Temel Eczacılık Bilimleri, Eczacılık, Yaşam Bilimleri, Moleküler Biyoloji ve Genetik, Sitogenetik, Kimya, Biyokimya, Alkoloidler, Sağlık Bilimleri, Diğer, Temel Bilimler, Basic Pharmaceutics Sciences, Pharmacology and Therapeutics, Life Sciences, Molecular Biology and Genetics, Cytogenetic, Chemistry, Biochemistry, Alcaloides, Health Sciences, Other, Natural Sciences, BİYOKİMYA VE MOLEKÜLER BİYOLOJİ, Yaşam Bilimleri (LIFE), KİMYA, UYGULAMALI, Temel Bilimler (SCI), KİMYA, TIBBİ, KİMYA, MULTİDİSİPLİNER, FARMAKOLOJİ VE ECZACILIK, Farmakoloji ve Toksikoloji, BIOCHEMISTRY & MOLECULAR BIOLOGY, MOLECULAR BIOLOGY & GENETICS, Life Sciences (LIFE), CHEMISTRY, APPLIED, CHEMISTRY, Natural Sciences (SCI), CHEMISTRY, MEDICINAL, CHEMISTRY, MULTIDISCIPLINARY, PHARMACOLOGY & PHARMACY, PHARMACOLOGY & TOXICOLOGY, Farmakoloji, İlaç Keşfi, Farmakoloji, Toksikoloji ve Eczacılık (çeşitli), Genel Farmakoloji, Toksikoloji ve Eczacılık, Farmakoloji (tıbbi), İlaç Rehberleri, Kimya (çeşitli), Genel Kimya, Proses Kimyası ve Teknolojisi, Yapısal Biyoloji, Moleküler Biyoloji, Klinik Biyokimya, Kanser Araştırmaları, Yaşlanma, Biyokimya, Genetik ve Moleküler Biyoloji (çeşitli), Genel Biyokimya, Genetik ve Moleküler Biyoloji, Fizik Bilimleri, Pharmacy, Pharmacology, Drug Discovery, Pharmacology, Toxicology and Pharmaceutics (miscellaneous), General Pharmacology, Toxicology and Pharmaceutics, Pharmacology (medical), Drug Guides, Chemistry (miscellaneous), General Chemistry, Process Chemistry and Technology, Structural Biology, Molecular Biology, Clinical Biochemistry, Cancer Research, Aging, Biochemistry, Genetics and Molecular Biology (miscellaneous), General Biochemistry, Genetics and Molecular Biology, Physical Sciences, 1,2,4-Triazole, Atropisomer, Diastereotope, X-ray diffraction, Cancer, Angiogenesis, mPGES-1, Cytotoxicity, PROSTAGLANDIN-E SYNTHASE-1, ANTIINFLAMMATORY ACTIVITY, HYBRIDS SYNTHESIS, BETA-CATENIN, TUMOR-GROWTH, DERIVATIVES, COX-2, DISCOVERY, DESIGN, ANTIBACTERIAL
Citation
Bulbul 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