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

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

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

机译：一些二价对称5取代的乙烯蛋白衍生物朝向人脑胶质瘤U251细胞（U251）和人癌细胞（KB3-1）的抗增殖活性

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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 lb 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 mu M, 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 lb 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.

机译：使用人脑胶质瘤细胞系（U251）和人癌细胞系（KB3-1）在体外评估新的二价双药型乙藻衍生物。在本研究中检查的5-取代的乙烯素衍生物（1A-B和2A-D）中，二价对称的5-取代的羟基衍生物LB朝向U251和KB3-1细胞显示出最高的抗增殖活性。该乙素衍生物对两种细胞系（U251和KB3-1）的抗增殖活性（IC50）的值分别为0.46和5.21μm。除了对U251细胞的化合物2a和2d外，所有化合物的抗增殖活性高于顺铂。二价对称化合物LB在分子中具有联苯甲烷接头。所有测试的二价候补素衍生物表现出对U251细胞的较高活性而不是抗KB3-1细胞。对于在分子中具有线性亚甲基接头的双药型乙炔衍生物2A-D，发现这些分子中的亚甲基接头长度对U251和KB3-1细胞的抗增殖活性有影响。

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来源
《Biological & pharmaceutical bulletin》 |2019年第11期|共4页
作者
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;
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作者单位

Fukuoka Univ Fac Pharmaceut Sci Jonan Ku 8-19-1 Nanakuma Fukuoka Fukuoka 8140180 Japan;

Fukuoka Univ Fac Pharmaceut Sci Jonan Ku 8-19-1 Nanakuma Fukuoka Fukuoka 8140180 Japan;

Fukuoka Univ Fac Pharmaceut Sci Jonan Ku 8-19-1 Nanakuma Fukuoka Fukuoka 8140180 Japan;

Univ Miyazaki Hosp Dept Pharm 5200 Kihara Kiyotake Miyazaki 8891692 Japan;

Univ Miyazaki Hosp Dept Pharm 5200 Kihara Kiyotake Miyazaki 8891692 Japan;

Univ Miyazaki Hosp Dept Pharm 5200 Kihara Kiyotake Miyazaki 8891692 Japan;

Kagoshima Univ Hosp 8-35-1 Sakuragaoka Kagoshima 8908520 Japan;

Sojo Univ Fac Pharmaceut Sci Nishi Ku 4-22-1 Ikeda Kumamoto 8600082 Japan;

Sojo Univ Fac Pharmaceut Sci Nishi Ku 4-22-1 Ikeda Kumamoto 8600082 Japan;

Fukuoka Univ Fac Pharmaceut Sci Jonan Ku 8-19-1 Nanakuma Fukuoka Fukuoka 8140180 Japan;

Fukuoka Univ Fac Pharmaceut Sci Jonan Ku 8-19-1 Nanakuma Fukuoka Fukuoka 8140180 Japan;

Fukuoka Univ Fac Pharmaceut Sci Jonan Ku 8-19-1 Nanakuma Fukuoka Fukuoka 8140180 Japan;

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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
hydantoin; symmetrical bivalent molecule; anti-proliferative activity; U251 cell; KB3-1 cell; cytotoxic activity;

机译：杜娟素;对称二价分子;抗增殖活动;U251细胞;KB3-1细胞;细胞毒性活性;

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1. B7-H4 expression is elevated in human U251 glioma stem-like cells and is inducible in monocytes cultured with U251 stem-like cell conditioned medium [J] . Lian-Jie Mo, Hong-Xing Ye, Ying Mao, 癌症（英文版） . 2013,第012期
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4. Cathepsin L suppression increases the radiosensitivity of human glioma U251 cells via G2/M cell cycle arrest and DNA damage [J] . Qing-qing ZHANG, Wen-juan WANG, Jun LI, 中国药理学报：英文版 . 2015,第009期
5. Anti-proliferative Activities towards Human Brain Glioma U251 Cells and Human Carcinoma Cells (KB3-1) of Some Twin-Drug Type Bivalent C-2-Symmetrical Phenylboronic Acid Derivatives [J] . Furutachi Makoto, Gondo Toshiaki, Ikeda Ryuji, Biological & pharmaceutical bulletin . 2019,第5期

机译：对人脑胶质瘤U251细胞和人癌细胞（KB3-1）的抗增殖活动，一些双药物二价C-2- 2-对称苯基硼酸衍生物
6. Anti-proliferative Activities towards Human Brain Glioma U251 Cells and Human Carcinoma Cells (KB3-1) of Some Twin-Drug Type Bivalent C-2-Symmetrical Phenylboronic Acid Derivatives [J] . Furutachi Makoto, Gondo Toshiaki, Ikeda Ryuji, Biological & pharmaceutical bulletin . 2019,第5期

机译：对人脑胶质瘤U251细胞和人癌细胞（KB3-1）的抗增殖活动，一些双药物二价C-2- 2-对称苯基硼酸衍生物
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机译：从草培养的灵芝分离的多糖肽在人U251胶质瘤细胞系中诱导抗增殖和促凋亡作用
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机译：新城疫病毒触发U251胶质瘤细胞自噬以增强病毒复制
9. The anti-cancer activities of Paeoniae Radix extracts on human hepatocellular carcinoma cell-line HepG2 and multidrug resistant human hepatocellular carcinoma cell-line R-HepG2 and their action mechanisms. [D] . Li, Lok Yee Mandy. 2004

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10. Polysaccharide peptide isolated from grass-cultured Ganoderma lucidum induces anti-proliferative and pro-apoptotic effects in the human U251 glioma cell line [O] . Chunhua Wang, Dongmei Lin, Quan Chen, -1

机译：从草培养的灵芝中分离出的多糖肽在人U251胶质瘤细胞系中诱导抗增殖和促凋亡作用
11. Differential pro-apoptotic effects of synthetic 4-thiazolidinone derivative Les-3288, doxorubicin and temozolomide in human glioma U251 cells [O] . Lesya I. Коbylinska, Olga Yu. Klyuchivska, Iryna I. Grytsyna, 2017

机译：合成的4-噻唑烷酮衍生物LES-3288，人胶质瘤U251细胞中的血栓蛋白衍生物LES-3288，多柔比蛋白和替替唑胺的差异促凋亡作用
12. Antibody-Dependent Cell-Mediated Antibacterial Activity of Human Mononuclear Cells. I. K Lymphocytes and Monocytes are Effective against Meningococci in Cooperation with Human Immune Sera [R] . Lowell, G. H., Smith, L. F., Artenstein, M. S., 1979

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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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