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
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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DOI：
10.1248/bpb.b18-00859
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发表时间：
2019-05-01
影响因子：
2
通讯作者：
Sumoto, Kunihiro
中科院分区：
文献类型：
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作者：
Furutachi, Makoto;Gondo, Toshiaki;Sumoto, Kunihiro
C-2-对称二价苯基硼酸衍生物具有多种显着的生物活性，如抗单纯疱疹病毒（HSV）-1和针对Vero细胞的细胞毒活性，并且可以逆转抗癌药物的作用。合成了新型对称二价分子，并使用人脑胶质瘤细胞系（U251）和人癌细胞系（KB3-1）在体外评估了它们的生物活性。在测试的化合物(1a-i)中，二价C-2-对称苯基硼酸衍生物Ig对U251和KB3-1细胞均表现出最高的抗增殖活性。该化合物对两种细胞系(U251和KB3-1)的50％抗增殖活性(IC50)值分别为19.0和3.78μM。化合物1g对KB3-1细胞的抗增殖活性高于顺铂。二价C-2-对称化合物1g在分子中具有线性亚甲基连接体。
Derivatives of C-2-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 C-2-symmetrical phenylboronic acid derivative Ig 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 mu M, respectively. The anti-proliferative activity of compound 1g towards KB3-1 cells was higher than that of cisplatin. The bivalent C-2-symmetrical compound 1g had a linear methylene linker in the molecule.