Yazar "Sağlam, Mehmet F." seçeneğine göre listele

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    Dimethoxyindoles based thiosemicarbazones as multi-target agents; synthesis, crystal interactions, biological activity and molecular modeling
    (Academic Press Inc Elsevier Science, 2022) Yıldız, Minhal; Bingül, Murat; Zorlu, Yunus; Sağlam, Mehmet F.; Boğa, Mehmet; Temel, Mutesir; Şengül, İbrahim F.; Kandemir, Hakan
    Alzheimer's disease (AD) is known as one of the most devastating neurodegenerative disease diagnosed for the old-aged people and cholinesterase inhibitors (ChEI) can be used as an effective palliative treatment for AD. A range of novel monomeric and dimeric indole based thiosemicarbazone derivatives 17-28 was synthesized in order to target cholinesterases (ChE). Biological importance of the targeted compounds 17-28 was investigated by employing the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes along with three different antioxidant property determination assays, namely DPPH free radical scavenging, ABTS cationic radical decolarization, and CUPRAC cupric reducing antioxidant capacity. The compounds 18 and 19 displayed the best inhibitor activity against BChE with IC50 values of 7.42 and 1.95 mu M, respectively. The antioxidant potentials were found to be moderate for DPPH and ABTS assays and the compounds 28 and 18 were the most potent candidates for both antioxidant assays. Cupric reducing capacity was the most promising assay and the compounds 25, 26 and 28 provided better inhibition values than all the standards. Further binding mode and affinity studies performed by molecular docking and molecular dynamics simulations. Accordingly, the compound 19 is the most plausible candidate that can compete with galantamine (GNT), a common pharmaceutics targeting both cholinesterase enzymes.
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    Investigation of spectroscopic properties of mono and Di-styryl indole-containing BODIPYs
    (Elsevier B.V., 2023) Topaloğlu Aksoy, B.; Erol, İsmail; Kandemir, Hakan; Sağlam, Mehmet F.; Şengül, I.F.; Çoşut, B.
    In the current study, two novel mono- and distyryl BODIPYs have been successfully synthesized employing the Knoevenagel type condensation reaction between 1,3,5,7?tetramethyl BODIPY and 2,3-diphenyl-4,6-dimethoxyindole-7-carbaldehyde. This C[sbnd]C bond extension approach leads to change in hybridization of methyl carbon from sp3 to sp2 which play quite important role in the photophysical properties of BODIPYs by allowing extended conjugation. The absorption and fluorescence spectroscopy were used to determine the photophysical properties include molar extinction coefficient, fluorescence lifetime and fluorescence quantum yield. Moreover, the effect of solvent polarity on targeted BODIPY units were analysed with experimental investigations. The Density Functional Theory (DFT)-optimized structures were consisted with the experimental data obtained from the single-crystal X-ray structures. © 2022 Elsevier B.V.
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    Methoxy-activated indole-7-carbohydrazides; synthesis, antioxidant, and anticancer properties
    (Wiley, 2022) Kandemir, Hakan; Izgi, Samet; Çınar, İrfan; Cebeci, Fatma; Dirican, Ebubekir; Sağlam, Mehmet F.; Şengül, İbrahim F.
    Indole has been known as a key heterocyclic motif in the development of new structures for both chemical and biological properties. In this current study, a new range of indole-7-carbohydrazides has been successfully synthesized starting from the readily available 3-phenyl and 2,3-diphenyl 4,6-dimethoxyindoles. The structures of the novel compounds were confirmed by utilizing H-1 NMR, C-13 NMR, FT-IR, high-resolution mass spectrometry, and single crystal X- ray diffraction techniques. In addition, the indole-7-carbohydrazides showed promising antioxidant results in preliminary screens. Some of the new compounds generated from dimethoxy indoles were also screened for their anticancer activity against SH-SHY5Y (human neuroblastoma), AGS (human gastric adenocarcinoma), and MDA-MB-231 (human breast adenocarcinoma) cell lines. The results revealed that the compound 12 was the promising candidate, showing cytotoxic effects on both neuroblastoma, stomach, and breast cancer cells.