Anti-proliferative Activities towards Human Brain Glioma U251 Cells and Human Carcinoma Cells (KB3-1) of Some Twin-Drug Type Bivalent <i>C</i><sub>2</sub>-Symmetrical Phenylboronic Acid Derivatives
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- Furutachi Makoto
- Faculty of Pharmaceutical Sciences, Fukuoka University
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- Gondo Toshiaki
- 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
Bibliographic Information
- Other Title
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- Anti-proliferative Activities towards Human Brain Glioma U251 Cells and Human Carcinoma Cells (KB3-1) of Some Twin-Drug Type Bivalent C₂-Symmetrical Phenylboronic Acid Derivatives
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Abstract
<p>Derivatives of C2-symmetrical bivalent phenylboronic acid exhibit several remarkable biological activities such as anti-herpes simplex virus (HSV)-1 and cytotoxic activities against Vero cells and they can reverse the effect of anticancer drugs. Novel symmetrical bivalent molecules were synthesized and their biological activities were evaluated in vitro using a human brain glioma cell line (U251) and a human carcinoma cell line (KB3-1). Among the tested compounds (1a–i), bivalent C2-symmetrical phenylboronic acid derivative 1g showed the highest anti-proliferative activity towards both U251 and KB3-1 cells. The values of 50% anti-proliferative activity (IC50) of this compound against the two cell lines (U251 and KB3-1) were 19.0 and 3.78 µM, respectively. The anti-proliferative activity of compound 1g towards KB3-1 cells was higher than that of cisplatin. The bivalent C2-symmetrical compound 1g had a linear methylene linker in the molecule.</p>
Journal
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- Biological and Pharmaceutical Bulletin
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Biological and Pharmaceutical Bulletin 42 (5), 833-836, 2019-05-01
The Pharmaceutical Society of Japan