Goal: 08 - İnsana Yakışır İş ve Ekonomik Büyüme
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İnsana Yakışır İş ve Ekonomik Büyüme
İstikrarlı, kapsayıcı ve sürdürülebilir ekonomik büyümeyi, tam ve üretken istihdamı ve herkes için insana yakışır işleri desteklemek
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Publication Metadata only Synthesis and Comprehensive in Vivo Activity Profiling of Olean-12-en-28-ol, 3β-Pentacosanoate in Experimental Autoimmune Encephalomyelitis: A Natural Remyelinating and Anti-Inflammatory Agent(2023-01-01) Şenol H.; Özgün Acar Ö.; Dağ A.; Eken A.; Güner H.; Aykut Z. G.; Topçu G.; Şen A.; ŞENOL, HALIL; DAĞ, AYDAN; TOPÇU, GÜLAÇTIPublication Metadata only Synthesis, Characterization and Molecular Docking Studies of Highly Selective New Hydrazone Derivatives of Anthranilic Acid and Their Ring Closure Analogue Quinazolin-4(3H)-ones Against Lung Cancer Cells A549(2023-02-01) Tokalı F. S.; Şenol H.; Bulut Ş.; Hacıosmanoğlu Aldoğan E.; ŞENOL, HALILPublication Metadata only Synthesis, characterization, molecular docking and in vitro anti-cancer activity studies of new and highly selective 1,2,3-triazole substituted 4-hydroxybenzohyrdazide derivatives(2023-02-01) Şenol H.; Ağgül A. G.; Atasoy S.; Güzeldemirci N.; ŞENOL, HALIL; ATASOY, SEZENPublication Open Access Synthesis and Evaluation of Quinazolin-4(3H)-one Derivatives as Multitarget Metabolic Enzyme Inhibitors: A Biochemistry-Oriented Drug Design(2023-07-01) Tokalı F. S.; Taslimi P.; Sadeghi M.; Şenol H.; ŞENOL, HALILIn this study, imines bearing quinazolin-4(3H)-one were synthesized and their inhibitory properties were investigated against some metabolic enzymes including Acetylcholinesterase (AChE), Butyrylcholinesterase (BChE), & alpha;-Glycosidase (& alpha;-Gly), and human Carbonic Anhydrase I-II (hCA I-II). All compounds had inhibitory strength with K-i values in the range of 38.55 & PLUSMN;4.08-159.05 & PLUSMN;10.68 nM and 41.04 & PLUSMN;6.73-177.12 & PLUSMN;8.06 nM against hCA I and hCA-II, respectively in comparison to the standard acetazolamide (AZA) K-i=125.15 & PLUSMN;0.78 nM (for hCA-I) and K-i=148.75 & PLUSMN;0.92 nM (for hCA-II). The compounds showed potent inhibitory activity against & alpha;-Gly enzyme with IC50 value 0.34-2.28 nM (standard inhibitor acarbose (ACR): 3.18 nM). Also, these analogs had potent inhibitory strength with K-i values in the range of 4.20 & PLUSMN;0.15-26.10 & PLUSMN;2.36 nM against AChE and 1.22 & PLUSMN;0.05-16.09 & PLUSMN;0.88 nM against BChE in comparison to the standard tacrine (TAC) K-i=37.62 & PLUSMN;6.86 nM (for AChE) and K-i=26.75 & PLUSMN;5.79 nM (for BChE). Additionally, the molecular docking and molecular dynamics simulation study was carried out for the determination of ligand-enzyme interactions. The docking scores of the most active compound were calculated as -7.31, -7.59, -6.66, -6.93 and -7.11 kcal/mol for AChE, BChE, hCA I, hCA II, and & alpha;-Gly, respectively.Publication Metadata only Novel Thiosemicarbazone and Thiazolidin‐4‐one Derivatives Containing Vanillin Core: Synthesis, Characterization and Anticancer Activity Studies(2023-01-01) Tokalı F. S.; Şenol H.; Dağ A.; Gençoğlu Katmerlikaya T.; Şendil K.; ŞENOL, HALIL; DAĞ, AYDANPublication Open Access Synthesis and anticancer activity of novel derivatives of α,β‐unsaturated ketones based on oleanolic acid: in vitro and in silico studies against prostate cancer cells(2023-08-01) Şenol H.; Ghaffari-Moghaddam M.; Bulut Ş.; Akbaş F.; Köse A.; Topçu G.; ŞENOL, HALIL; AKBAŞ, FAHRİ; TOPÇU, GÜLAÇTIHerein, new derivatives of α,β-unsaturated ketones based on oleanolic acid (4 a-i) were designed, synthesized, characterized, and tested against human prostate cancer (PC3). According to the in vitro cytotoxic study, title compounds (4 a-i) showed significantly lower toxicity toward healthy cells (HUVEC) in comparison with the reference drug doxorubicin. The compounds with the lowest IC50 values on PC3 cell lines were 4 b (7.785 μM), 4 c (8.869 μM), and 4 e (8.765 μM). The results of the ADME calculations showed that the drug-likeness parameters were within the defined ranges according to Lipinski's and Jorgensen's rules. For the most potent compounds 4 b, 4 c, and 4 e, a molecular docking analysis using the induced fit docking (IFD) protocol was performed against three protein targets (PARP, PI3K, and mTOR). Based on the IFD scores, compound 4 b had the highest calculated affinity for PARP1, while compound 4 c had higher affinities for mTOR and PI3K. The MM-GBSA calculations showed that the most potent compounds had high binding affinities and formed stable complexes with the protein targets. Finally, a 50 ns molecular dynamics simulation was performed to study the behavior of protein target complexes under in silico physiological conditions.Publication Metadata only Mediator role of innovation in the relationship between social development and happiness(2023-12-01) Gözübol Z. İ.; Baysal Yiğit A.; Toker K.; GÖZÜBOL, ZEKİYE İREM; TOKER, KEREMGovernments, organizations, and researchers discuss the policies necessary for people and societies to lead a happy life in the 21st century as a critical issue. Although researchers expect a positive relationship between the happiness levels of communities and their social development levels, it is necessary to question the direction, the strength of this relationship and the existence of different variables affecting it. In this context, in this study, we aimed to examine the relationships among societies’ development level, happiness level, and innovation capacity. For this purpose, we obtained 2020 data from global reports covering the social development, innovation, and happiness variables of 119 countries. We tested the research model within the framework of these data and hierarchical regression analysis, and we found that innovation partially mediates the relationship between the social development levels of countries and happiness. Research results show that innovation is an intellectual and industrial process that positively affects the happiness of societies