1. Anti-proliferative Activities of Some Bivalent Symmetrical 5-Substituted Hydantoin Derivatives towards Human Brain Glioma U251 Cells (U251) and Human Carcinoma Cells (KB3-1)
- Author
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Tsubasa Yokota, Yasuo Takeda, Naoki Yoshikawa, Jian-Rong Zhou, Fumio Miake, Nobuhiro Kashige, Kaori Ota, Makoto Furutachi, Kazumi Yokomizo, Ryuji Ikeda, Fumiko Fujisaki, and Kunihiro Sumoto
- Subjects
0301 basic medicine ,Stereochemistry ,Pharmaceutical Science ,Hydantoin ,Antineoplastic Agents ,Bivalent (genetics) ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Cell Line, Tumor ,medicine ,Humans ,Methylene ,IC50 ,Cell Proliferation ,Pharmacology ,Cisplatin ,Molecular Structure ,Hydantoins ,General Medicine ,In vitro ,030104 developmental biology ,chemistry ,Cell culture ,030220 oncology & carcinogenesis ,Linker ,medicine.drug - Abstract
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.
- Published
- 2019
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