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  • Küçük Resim
    Öğe
    Synthesis, structural characterization and myorelaxant activity of 4-naphthylhexahydroquinoline derivatives containing different ester groups
    (Serbian Chemical Soc, 2016) Gunduz, Miyase Gozde; Albayrak, Emine; Isli, Fatma; Fincan, Gokce Sevim Ozturk; Yildirim, Seniz; Simsek, Rahime; Butcher, Ray J.
    The present study reports the synthesis, structural characterization and myorelaxant activity evaluation of a series of 16 novel 4-naphthylhexahydroquinoline derivatives. The compounds were achieved by one-pot microwave-assisted method via a modified Hantzsch reaction. The structures of the compounds were confirmed by various spectral methods, such as IR, 1D and 2D NMR techniques and mass analysis. X-Ray studies of compound 10 provided further evidence for the proposed structure. To evaluate their myorelaxant activities, the E-max and pD(2) values of the compounds and nifedipine were determined on isolated rabbit gastric fundus smooth muscle strips. The obtained results indicated that the introduction of long chain alkyl groups, such as the 2-methoxyethyl or 2-(methacryloyloxy)ethyl moiety, to the ester group led to the most active compounds.
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    Öğe
    The Synthesis and Anti-cancer Activities of Ferrocenyl Chalcones; Drug-Likeness Calculations
    (Kırıkkale Üniversitesi, 2021) Albayrak, Emine; Işılar, Özer; Bıyıkoğlu, Mutluhan; Şahin Yağlıoğlu, Ayşe; Bulut, Adnan
    A series of 1-8 different ferrocenyl chalcones were synthesized through the Claisen–Schmidt condensation and the Friedel?Crafts acylation. Their structures were confirmed by means of 1H, 13C NMR and FT-IR. The cytotoxic and antiproliferative activities of the chalcones were screened against HeLa (cervix cancer) and PC3 (prostate cancer) cell lines. They showed excellent anti-cancer activities especially against PC3 cell even at very low concentration (5 µM). Also, their physicochemical properties, drug-likeness calculations and the rule of five (RO5) were investigated.