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    Anticancer Activity-Structure Relationship of Quinolinone-Core Compounds: An Overall Review
    (Springer, 2023) Beker, Hueseyin Kerim; Yildirim, Isil
    Quinolinone/quinoline is one of the most unique structures in the discovery of heterocycles that have attracted much attention in the field of medicinal chemistry. The basic scaffold of fused quinoline derivatives is of great interest to medicinal chemists since large road maps of the gene and protein expression can be used to classify cancers or predict responses to certain types of treatments targeting the level of both transcription and translation and the level of enzyme activity. These specific regulations may open the door for the discovery of new drug candidates including anticancer targets. This review provides a comprehensive description of various quinolinone derivatives, especially by concentrating on compounds containing benzimidazole rings. Quinolone moieties are experimentally proven anticancer pharmacophores which may further enhance their activity due to various functional groups, mostly the electron-withdrawing groups such as fluoro, chloro, nitro, amino, and carbonyl groups that showed stronger activity than those with electron-donating groups such as methyl and methoxy groups. The presence of an electron-withdrawing or electron-donating group at the quinolone ring influences the redox properties affecting DNA synthesis. Structural motifs attributed to noteworthy inhibitory results are identified and highlighted to encourage further research and drug development. This work aims to help researchers in discovering more powerful, active, and less toxic quinoline-based anticancer drugs and developing new vision in the search for their rational design.
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    One-pot Multicomponent Reaction: An Efficient Synthesis of 4-(Het)Aryl-substituted Pyrazolo-quinolinones
    (Bentham Science Publ Ltd, 2024) Beker, Hueseyin Kerim; Kaban, Seniz
    Introduction Pyrazolo-quinolinones (PQs) are a versatile class of Organic chemistry and it was found that they have very advanced functionally promising as selective compounds due to their scaffold and demonstrated low toxicity and considerable clinical promise. Moreover, these compounds have an important role in different applications such as analytical reagents, technical, pharmaceutical development, and biological markers. So, we aimed to synthesize and characterize new 4-(Het)aryl-substituted Pyrazole-quinolinones.Methods Synthesis of One-Pot Multicomponent Reaction was carried out with the reaction of 5-amino-3-methyl-1H-pyrazole 1a, and 5-amino-3-phenyl-1H-pyrazole 1b and dimedone 2 with some (het)aryl aldehydes 3 using ethanol. Characterizations such as the linear structures and the regiospecificity of the reactions were determined by using NMR, GC-MS, IR, and UV measurements.Results and Conclusion This research will be very useful for all methods and procedures using multi one-point reactions which are very popular in the synthesis of heterocyclic systems for pyrazole- quinoline skeleton synthesis.