Yazar "Tekin, Saban" seçeneğine göre listele

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  • Küçük Resim
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    Detection of mechanism and anticancer activity of the new quinoline compounds MC20 and MC21
    (Elsevier Science Bv, 2014) Koprulu, Tugba Kul; Tekin, Saban; Okten, Salih; Cinar, Merve; Duman, Seda; Cakmak, Osman
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  • Küçük Resim
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    Determination of anticancer activities of some quinoline derivatives against C6 tumor cells
    (Elsevier Science Bv, 2012) Sahin, Onem Yuce; Okten, Salih; Tekin, Saban; Cakmak, Osman
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  • Küçük Resim
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    In vitro antiproliferative/cytotoxic activity of 2,3 '-biindole against various cancer cell lines
    (Tubitak Scientific & Technical Research Council Turkey, 2015) Okten, Salih; Erenler, Ramazan; Koprulu, Tugba Kul; Tekin, Saban
    2,3'-Biindole (2) was synthesized via bromination of indole (1) with molecular bromine and underwent simultaneous dimerization. Antiproliferative and cytotoxic activity of 2 was investigated in vitro on C6 (rat brain tumor), HeLa (human cervix carcinoma), and HT29 (human colon carcinoma) cells lines by using BrdU cell proliferation ELISA and lactate dehydrogenase (LDH) assays. In contrast to 5-fluorouracil (5-FU), 2,3'-biindole (2) significantly inhibited proliferation of HeLa and HT29 cell lines. According to LDH assay, the cytotoxicity of compound 2 was low on HT29 cell lines and high on HeLa and C6 cell lines. Moreover, 2 did not cause any DNA laddering on the DNA of tested cells; therefore, it is suggested that the mechanism of action of this compound may not involve apoptosis. In addition, 2 inhibited relaxation of supercoiled plasmid DNA by topoisomerase activity. Results of the present study indicates that biindole (2) may have promising anticancer and antitopoisomerase potential with an unknown mechanism of action.
  • Küçük Resim
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    In vitro antiproliferative/cytotoxic activity of novel quinoline compound SO-18 against various cancer cell lines
    (Elsevier Science Bv, 2014) Okten, Salih; Sahin, Onem Yuce; Tekin, Saban; Cakmak, Osman
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  • Küçük Resim
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    A SAR Study: Evaluation of Bromo Derivatives of 8-Substituted Quinolines as Novel Anticancer Agents
    (Bentham Science Publ Ltd, 2017) Okten, Salih; Cakmak, Osman; Tekin, Saban; Koprulu, Tugba Kul
    Background: Brominated 8-hydroxy, 8-methoxy, 8-amino quinolines 5, 6, 8, 9 and novel cyano 8-hydroxyquinolines 11, 12 were evaluated in vitro for their anticancer effects on various cell lines. 5,7-Dibromo-5, 7-bromo-6, 7-cyano-11 and 5,7-dicyano-12 8-hydroxyquinolines were shown to have strong antiproliferative activity against various tumor cell lines, including C6 (rat brain tumor), HeLa (human cervix carcinoma), and HT29 (human colon carcinoma) with IC50 values ranged from 6.7 to 25.6 mu g/mL. Methods: A structure activity relationship (SAR) was conducted that quinoline core containing hydroxly group at C-8 positon led to more anti cancer potentials. Results: The results of Lactate Dehydrogenase (LDH) cytotoxic, DNA laddering and inhibition assays indicated that 5, 6, 11 and 12 have high cytotoxic effects and appototic potentials. Conclusion: Furthermore, 5 and 12 have inhibitory effects on relaxation of supercoiled plazmid DNA by supressed the Topoisomerase I enzyme. As a result, 5, 6, 11 and 12 may have promising anticancer drug potential and 5 and 12 may be novel topoisomerase inhibitors.
  • Küçük Resim
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    Simple and convenient preparation of novel 6,8-disubstituted quinoline derivatives and their promising anticancer activities
    (Scientific Technical Research Council Turkey-Tubitak, 2013) Okten, Salih; Cakmak, Osman; Erenler, Ramazan; Yuce, Onem; Tekin, Saban
    A short and easy route is described for 6,8-disubstituted derivatives of quinoline and 1,2,3,4-tetrahydroquinoline from 6,8-dibromoquinolines 2 and 7 by various substitution reactions. While copper-promoted substitution of 6,8-dibromide 2 produced monomethoxides 3 and 4, a prolonged reaction time mainly afforded dimethoxide 6 instead of 5, whose aromatization with DDQ and substitution reaction of dibromide 7 with NaOMe in the presence of CuI also gave rise to dimethoxide 6. Several 6,8-disubstituted quinolines were obtained by treatment of 6,8-dibromoquinoline (7) with n-BuLi followed by trapping with an electrophile [Si(Me)(3)Cl, S-2(Me)(2), and DMF]. Furthermore, 7 was also converted to mono and dicyano derivatives. The anticancer activities of compounds 2, 7, 6, 12, 13, 15, and 16 against HeLa, HT29, and C6 tumor cell lines were tested, and 6,8-dibromo-1,2,3,4-tetrahydroquinoline (2) and 6,8-dimethoxyquinoline (6) showed significant anticancer activities against the tumor cell lines.