Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors

Gizem ERENSOY, (Marmara Üniversitesi, Eczacılık Fakültesi, Farmasötik Kimya Anabilim Dalı, Haydarpaşa 34668 İstanbul, Türkiyel)
Kai DING, (Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY 40536, United States)
Chang-Guo ZHAN, (Center for Pharmaceutical Research and Innovation, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY 40536, United States.)
Ammar ELMEZAYEN, (Kadir Has Üniversitesi, Mühendislik ve Doğa Bilimleri Fakültesi, Biyoinformatik ve Genetik Bölümü, İstanbul, Türkiye)
Kemal YELEKÇİ, (Kadir Has Üniversitesi, Mühendislik ve Doğa Bilimleri Fakültesi, Biyoinformatik ve Genetik Bölümü,İstanbul, Türkiye)
Merve DURACIK, (Marmara Üniversitesi, Eczacılık Fakültesi, Biyokimya Anabilim Dalı, Haydarpaşa 34668 İstanbul, Türkiye.)
Özlem BİNGÖL ÖZAKPINAR, (Marmara Üniversitesi, Eczacılık Fakültesi, Biyokimya Anabilim Dalı, Haydarpaşa 34668 İstanbul, Türkiye.)
İlkay KÜÇÜKGÜZEL (Marmara Üniversitesi, Eczacılık Fakültesi, Farmasötik Kimya Anabilim Dalı, Haydarpaşa 34668 İstanbul, Türkiye)
Journal of research in pharmacy (online)
1 0
Yıl: 2020 Cilt: 24 Sayı: 4 Sayfa Aralığı: 436 - 451 Metin Dili: İngilizce DOI: 10.35333/jrp.2020.187 İndeks Tarihi: 10-10-2020

Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors

Öz:
A series of new 1,3,4-oxadizole derivatives containing thioether group, has been synthesized to investigate their mPGES-1 inhibitory activities. The synthesized compounds were also evaluated for their anticancer and COX-1/2 inhibitory activities. All compounds were checked for their purity using TLC and HPLC analyses. The melting points, elemental analysis, FT-IR, 1H-/13C-NMR and LR-MS data were utilized for structural characterization.The most potent derivative was 2-[5-{[2-methyl-5-(propan-2-yl)phenoxy]methyl}-1,3,4-oxadiazol-2-yl)sulphanyl]-1-(phenyl)ethan-1-one 3a, which showed inhibitory activity against mPGES-1 with an IC50 of 4.95 μM. Docking studies with mPGES-1 and COX-1/2 enzymes revealed their affinity and potential binding mechanism for the testedcompounds.
Anahtar Kelime:

Belge Türü: Makale Makale Türü: Araştırma Makalesi Erişim Türü: Erişime Açık
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APA ERENSOY G, DING K, ZHAN C, ELMEZAYEN A, YELEKÇİ K, DURACIK M, Bingöl Özakpınar Ö, Küçükgüzel İ (2020). Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors. , 436 - 451. 10.35333/jrp.2020.187
Chicago ERENSOY Gizem,DING Kai,ZHAN Chang-Guo,ELMEZAYEN Ammar,YELEKÇİ Kemal,DURACIK Merve,Bingöl Özakpınar Özlem,Küçükgüzel İlkay Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors. (2020): 436 - 451. 10.35333/jrp.2020.187
MLA ERENSOY Gizem,DING Kai,ZHAN Chang-Guo,ELMEZAYEN Ammar,YELEKÇİ Kemal,DURACIK Merve,Bingöl Özakpınar Özlem,Küçükgüzel İlkay Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors. , 2020, ss.436 - 451. 10.35333/jrp.2020.187
AMA ERENSOY G,DING K,ZHAN C,ELMEZAYEN A,YELEKÇİ K,DURACIK M,Bingöl Özakpınar Ö,Küçükgüzel İ Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors. . 2020; 436 - 451. 10.35333/jrp.2020.187
Vancouver ERENSOY G,DING K,ZHAN C,ELMEZAYEN A,YELEKÇİ K,DURACIK M,Bingöl Özakpınar Ö,Küçükgüzel İ Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors. . 2020; 436 - 451. 10.35333/jrp.2020.187
IEEE ERENSOY G,DING K,ZHAN C,ELMEZAYEN A,YELEKÇİ K,DURACIK M,Bingöl Özakpınar Ö,Küçükgüzel İ "Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors." , ss.436 - 451, 2020. 10.35333/jrp.2020.187
ISNAD ERENSOY, Gizem vd. "Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors". (2020), 436-451. https://doi.org/10.35333/jrp.2020.187
APA ERENSOY G, DING K, ZHAN C, ELMEZAYEN A, YELEKÇİ K, DURACIK M, Bingöl Özakpınar Ö, Küçükgüzel İ (2020). Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors. Journal of research in pharmacy (online), 24(4), 436 - 451. 10.35333/jrp.2020.187
Chicago ERENSOY Gizem,DING Kai,ZHAN Chang-Guo,ELMEZAYEN Ammar,YELEKÇİ Kemal,DURACIK Merve,Bingöl Özakpınar Özlem,Küçükgüzel İlkay Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors. Journal of research in pharmacy (online) 24, no.4 (2020): 436 - 451. 10.35333/jrp.2020.187
MLA ERENSOY Gizem,DING Kai,ZHAN Chang-Guo,ELMEZAYEN Ammar,YELEKÇİ Kemal,DURACIK Merve,Bingöl Özakpınar Özlem,Küçükgüzel İlkay Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors. Journal of research in pharmacy (online), vol.24, no.4, 2020, ss.436 - 451. 10.35333/jrp.2020.187
AMA ERENSOY G,DING K,ZHAN C,ELMEZAYEN A,YELEKÇİ K,DURACIK M,Bingöl Özakpınar Ö,Küçükgüzel İ Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors. Journal of research in pharmacy (online). 2020; 24(4): 436 - 451. 10.35333/jrp.2020.187
Vancouver ERENSOY G,DING K,ZHAN C,ELMEZAYEN A,YELEKÇİ K,DURACIK M,Bingöl Özakpınar Ö,Küçükgüzel İ Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors. Journal of research in pharmacy (online). 2020; 24(4): 436 - 451. 10.35333/jrp.2020.187
IEEE ERENSOY G,DING K,ZHAN C,ELMEZAYEN A,YELEKÇİ K,DURACIK M,Bingöl Özakpınar Ö,Küçükgüzel İ "Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors." Journal of research in pharmacy (online), 24, ss.436 - 451, 2020. 10.35333/jrp.2020.187
ISNAD ERENSOY, Gizem vd. "Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors". Journal of research in pharmacy (online) 24/4 (2020), 436-451. https://doi.org/10.35333/jrp.2020.187
Sayfa Oluşturulma Tarihi
23-04-2024 13:44

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TÜBİTAK ULAKBİM TR Dizin

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