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AKDEMİR, ATİLLA

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Author: Akdemir A. × End date: 2023 × Start date: 2020 × Item Type: Publication × Rights: info:eu-repo/semantics/openAccess ×

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Now showing 1 - 4 of 4
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    Dithiocarbamates and dithiocarbonates containing 6-nitrosaccharin scaffold: Synthesis, antimycobacterial activity and in silico target prediction using ensemble docking-based reverse virtual screening
    (2022-12-01) Trawally M.; Demir Yazıcı K.; Dingiş Birgül S. İ.; Kaya K.; Akdemir A.; Güzel Akdemir Ö.; DİNGİŞ BİRGÜL, SERAP İPEK; AKDEMİR, ATİLLA
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    İlaç Tasarımı: Hedef Protein ile Etkileşimin Optimizasyonu
    (Nobel Tıp Kitapevi, 2021-01-01) Güzel Akdemir Ö.; Akdemir A.; AKDEMİR, ATİLLA
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    Aurone Scaffold and Structural Analogues for the Development of Monoamine Oxidase (MAO) Inhibitors
    (Bentham Science Publisher, 2022-12-01) Guglielmi P.; Pontecorvi V.; Akdemir A.; AKDEMİR, ATİLLA
    Medicinal chemists around the world have been inspired by nature and have successfully extracted chemicals from plants. Research on enzymatic modifications of naturally occurring compounds has played a critical role in the search for biologically active molecules to treat diseases. This book explores compounds of interest to researchers and clinicians. It presents a comprehensive analysis about the medicinal chemistry (drug design, structure-activity relationships, permeability data, cytotoxicity, appropriate statistical procedures, and molecular modeling studies) of different compounds. Each chapter brings contributions from known scientists explaining experimental results which can be translated into clinical practice. Each chapter follows a specific format for a phytochemical agent with common chemical features: • General background on the (phyto)chemistry of the scaffold • General background on the pharmacological profile of the scaffold • A Description of the proposed derivatives and their advantages with respect to the parent compounds (emphasizing the synthetic approaches and structure-activity relationships) • In silico analysis of the crucial interactions with the biological target • Clinical studies and patent survey (if available) on the new and proposed structures The objective of this book set is to fulfil gaps in currently acquired knowledge with information from the recent years. It serves as a guide for academic and professional researchers and clinicians.
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    Tail-Approach-Based Design and Synthesis of Coumarin-Monoterpenes as Carbonic Anhydrase Inhibitors and Anticancer Agents
    (2023-02-01) Kurt B. Z.; Celebi G.; Öztürk Civelek D.; Angeli A.; Akdemir A.; Sonmez F.; Supuran C. T.; ÖZTÜRK CİVELEK, DİLEK; AKDEMİR, ATİLLA; ZENGİN KURT, BELMA
    In this study, sixty novel coumarin-monoterpene compounds were synthesized in two series [thirty-two compounds (12-43) bearing a triazole ring in the first series, and twenty-eight compounds (44-71) bearing an alkyl chain in the second one]. Their inhibitory effects on the human carbonic anhydrase (hCA) isoforms I, II, IX, and XII and anticancer potentials were determined. All synthesized molecules selectively inhibited CA IX and XII. 23 and 42 were found to be the strongest inhibitors, with K i values of 1.9 nM against hCA IX. Also, 70 showed the highest inhibitory activity with a K i value of 4.9 nM against hCA XII. Moreover, their cytotoxic effects on colon adenocarcinoma (HT-29), prostate adenocarcinoma (PC-3), and breast adenocarcinoma (MCF-7) cell lines were evaluated. According to the cytotoxicity results, 14 (IC50 = 2.48 μM) and 63 (IC50 = 3.91 μM) exhibited the highest cytotoxicity on the MCF-7 cells, while 23 showed the strongest cytotoxic effect on both PC-3 (IC50 = 9.40 μM) and HT-29 (IC50 = 12.10 μM) cell lines. 14, 23, and 66 decreased CA IX and CA XII protein expression in HT-29 cells, while 23 and 66 showed the strongest reduction of both CA IX and CA XII in MCF-7 cells. All of the selected compounds increased total apoptosis in a concentration-dependent manner in HT-29 and MCF-7 cells. 14 has the strongest apoptotic effect in MCF-7 cells. 23 increased early apoptosis primarily, while 14 and 66 increased total apoptosis in HT-29. In addition, PI/Hoechst staining proves that apoptotic cells are increased in HT-29 with an effect of 14, 23, and 66. As a result of the modeling studies, it has been shown that only the open coumarin form of the compounds can interact directly with the active-site Zn2+ ion. It has been shown that coumarin-monoterpene structures with different alkyl and monoterpene groups both specifically inhibit CA IX and XII and exhibit specific cytotoxicity in different cell lines.