Anti-proliferative Activities of Some Bivalent Symmetrical 5-Substituted Hydantoin Derivatives towards Human Brain Glioma U251 Cells (U251) and Human Carcinoma Cells (KB3-1)

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 derivati...

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Published in:Biological & pharmaceutical bulletin 2019/11/01, Vol.42(11), pp.1953-1956
Main Authors: Furutachi, Makoto, Ota, Kaori, Fujisaki, Fumiko, Ikeda, Ryuji, Yoshikawa, Naoki, Yokota, Tsubasa, Takeda, Yasuo, Yokomizo, Kazumi, Zhou, Jian-Rong, Kashige, Nobuhiro, Miake, Fumio, Sumoto, Kunihiro
Format: Article
Language:English
Subjects:
anti-proliferative activity
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Brain
Cell Line, Tumor
Cell Proliferation - drug effects
Cisplatin
cytotoxic activity
Glioma
Glioma cells
Humans
Hydantoin
Hydantoins - chemistry
Hydantoins - pharmacology
KB3-1 cell
Methylene
Molecular Structure
symmetrical bivalent molecule
U251 cell
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Summary: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.
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.b19-00486