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DAĞ, AYDAN

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AYDAN
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DAĞ
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Has files: true × Start date: 2020 × End date: 2023 ×

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    PublicationOpen Access
    Synthesis and biological evaluation of novel coumarin-chalcone derivatives containing urea moiety as potential anticancer agents
    (2020-01-01T00:00:00Z) Kurt, BELMA; Kandas, Nur Ozten; DAĞ, AYDAN; Sonmez, Fatih; Kucukislamoglu, Mustafa; ZENGİN KURT, BELMA; DAĞ, AYDAN
    The increasing interest on new drug discovery is constantly up to date as drugs do not increase survival adequately against increasing cancer cases worldwide. Based on the reported anticancer activity of coumarin, chalcone and urea derivatives, the present investigation dealt with the design and synthesis of coumarin derivatives bearing diversely substituted chalcone-urea moieties 5a-k. Through a structure-based molecular hybridization approach, a series of novel coumarin-chalcone derivatives containing urea moiety was synthesized and screened for their in vitro antiproliferative activities against the cancer cell lines (H4IIE and HepG2). In addition, the synthesized compounds were tested on a cell line that was not cancerous (CHO) and the damage, it could give to normal cells was determined. Among the synthesized compounds, 5k exhibited better inhibition of H4IIE compared to Sorafenib. 5j also showed better inhibition against HepG2 than Sorafenib. In particular, 5k induced H4IIE apoptosis, arrested cell cycle at the S phase. Therefore, 5k and 5j may be potent antitumor agents, representing a promising lead for further optimization. (C) 2017 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University.
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    PublicationOpen Access
    GLUT-Targeting Phototherapeutic Nanoparticles for Synergistic Triple Combination Cancer Therapy.
    (2023-02-12T21:00:00Z) Cetin Ersen, Busra; Goncu, Beyza; Dag, Aydan; Birlik Demirel, Gokcen; DAĞ, AYDAN; GÖNCÜ, BEYZA SERVET
    The combination of multimodal therapies into one nanocarrier system is promising for its potential to enhance treatment performance by overcoming the efficacy problems encountered in conventional monomodal therapy. In this study, targeted and multimodal therapeutic hybrid nanocarriers are fabricated for breast cancer treatments. In this context, the synthesized gold nanorods (AuNRd), photothermal therapy (PTT) agent, are coated with doxorubicin (DOX) conjugated, targeted, and biocompatible tetrablock glycopeptide (P(DMAEMA--HMBAMA--FrucMA)--P(Lys)/DOX, P-DOX) polymer. Here, fructose-based (Fruc) glycopeptide polymer enhances cellular uptake into breast cancer through GLUT5. A photosensitizer molecule, indocyanine green (ICG), was loaded into the particles to provide photodynamic therapy (PDT) upon NIR light at 808 nm. In the final step of the fabrication, the polymer-coated nanoparticles are integrated with antisense ISIS5132 oligonucleotides to prevent apoptotic resistance of cells against drug molecules. The biocompatibility and therapeutic efficacy of the nanoparticles are evaluated on both human normal skin fibroblast cell (CCD-1079Sk) and human breast cancer cell (MCF7) lines. These multimodal therapeutic AuNRd@P-DOX/ICG/ISIS5132 nanoparticles demonstrate an efficient triple synergistic effect of chemo-/PTT/PDT, which is desired for breast cancer treatment. We believe that this promising multimodal therapeutic nanoparticle system can promote the further clinical application in the treatment of breast cancer and can also be adapted to other types of cancer.