Person:
AKDEMİR, ATİLLA

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ATİLLA
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AKDEMİR
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Now showing 1 - 4 of 4
  • PublicationMetadata only
    Design and synthesis of new heterocyclic compounds containing 5-[(1H-1,2,4-triazol-1-yl)methyl]-3H-1,2,4-triazole-3-thione structure as potent hEGFR inhibitors
    (2023-01-01) KOLCUOĞLU Y.; BEKİRCAN O.; Fazli H.; Sahin E.; TÜRE A.; AKDEMİR A.; Hamarat Sanlier S.; AKDEMİR, ATİLLA
    © 2023 Informa UK Limited, trading as Taylor & Francis Group.EGFR is one of the important mediators of the signaling cascade that determines key roles in various biological processes such as growth, differentiation, metabolism and apoptosis in the cell in response to external and internal stimuli. In recent years, it has been proven that although this enzyme activity is tightly regulated in normal cells, if the enzyme activity cannot be controlled, it can lead to malignancy. EGFR is also considered a prominent macromolecule in targeted cancer chemotherapy. For this purpose, a comprehensive modeling studies were conducted against EGFR protein and novel molecules containing 5-[(1H-1,2,4-triazol-1-yl)methyl]-3H-1,2,4-triazole-3-thione structure were suggested to be synthesized. Among the synthesized molecules, compounds 7c, 8c, 8f and 8g were determined to have significant IC50 values. Compound 8g was found to have the IC50 value closest to the very well-known EGFR inhibitor Gefitinib with its noncompetitive inhibition form. K i value of compound 8g was calculated as 0.00232 µM. Communicated by Ramaswamy H. Sarma.
  • PublicationMetadata only
    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
  • PublicationMetadata only
    İlaç Tasarımı: Hedef Protein ile Etkileşimin Optimizasyonu
    (Nobel Tıp Kitapevi, 2021-01-01) Güzel Akdemir Ö.; Akdemir A.; AKDEMİR, ATİLLA
  • PublicationMetadata only
    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.