Anti-proliferative Activities of Some Bivalent Symmetrical 5-Substituted Hydantoin Derivatives towards Human Brain Glioma U251 Cells (U251) and Human Carcinoma Cells (KB3-1)
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- Furutachi Makoto
- Faculty of Pharmaceutical Sciences, Fukuoka University
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- Ota Kaori
- Faculty of Pharmaceutical Sciences, Fukuoka University
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- Fujisaki Fumiko
- Faculty of Pharmaceutical Sciences, Fukuoka University
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- Ikeda Ryuji
- Department of Pharmacy, University of Miyazaki Hospital
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- Yoshikawa Naoki
- Department of Pharmacy, University of Miyazaki Hospital
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- Yokota Tsubasa
- Department of Pharmacy, University of Miyazaki Hospital
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- Takeda Yasuo
- Kagoshima University Hospital
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- Yokomizo Kazumi
- Faculty of Pharmaceutical Sciences, Sojo University
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- Zhou Jian-Rong
- Faculty of Pharmaceutical Sciences, Sojo University
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- Kashige Nobuhiro
- Faculty of Pharmaceutical Sciences, Fukuoka University
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- Miake Fumio
- Faculty of Pharmaceutical Sciences, Fukuoka University
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- Sumoto Kunihiro
- Faculty of Pharmaceutical Sciences, Fukuoka University
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Abstract
<p>Novel bivalent twin-drug type hydantoin derivatives were evaluated in vitro using a human brain glioma cell line (U251) and a human carcinoma cell line (KB3-1). Among the 5-substituted hydantoin derivatives (1a–b and 2a–d) examined in this study, bivalent symmetrical 5-substituted hydantoin derivative 1b showed the highest anti-proliferative activity towards both U251 and KB3-1 cells. The values of anti-proliferative activity (IC50) of this hydantoin derivative against the two cell lines (U251 and KB3-1) were 0.46 and 5.21 µM, respectively. The anti-proliferative activity of all of the compounds except for compounds 2a and 2d against U251 cells was higher than that of cisplatin. Bivalent symmetrical compound 1b had a biphenylmethane linker in the molecule. All of the tested bivalent hydantoin derivatives showed higher activity against U251 cells than against KB3-1 cells. For twin-drug type hydantoin derivatives 2a–d, which have a linear methylene linker in the molecules, it was found that methylene linker length in these molecules have an effect on the anti-proliferative activity against U251 and KB3-1 cells.</p>
Journal
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- Biological and Pharmaceutical Bulletin
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Biological and Pharmaceutical Bulletin 42 (11), 1953-1956, 2019-11-01
The Pharmaceutical Society of Japan