Anticancer activity of dinuclear gallium(III) carboxylate complexes
Anticancer activity of dinuclear gallium(III) carboxylate complexes
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DOI：
10.1016/j.ejmech.2009.10.038
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发表时间：
2010-02-01
影响因子：
6.7
通讯作者：
Kaluderovic, Goran N.
中科院分区：
文献类型：
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作者：
Kaluderovic, Milena R.;Gomez-Ruiz, Santiago;Kaluderovic, Goran N.
以3-甲氧基苯乙酸、4-甲氧基苯乙酸、均三甲苯硫代乙酸、2，5-二甲基-3-糠酸和1，4-苯并二氧六环-6-羧酸为原料，分别与三甲基镓（1：1）得到二聚配合物[Me_2Ga（μ-O2 CCH 2C 6 H4 -3-OMe）]（2）（1），[Me 2Ga（μ-O2 CCH 2C 6 H4 -4-OMe）]（2）（2），[Me 2Ga（mu-O（2）CCH（2）SMes）]（2）（3）（Mes = 2，4，6-Me 3C 6 H2），[Me 2Ga {μ-O2 C（Fur）}]（2）（4）（Fur = 2，5-二甲基呋喃）和[Me 2Ga {μ-O2 C（Bdo）}]（2）（5）（Bdo = 1，4-苯并二氧六环）。通过X射线衍射研究确定了5的分子结构。测试镓（III）配合物（1-5）对人肿瘤细胞系8505 C甲状腺未分化癌、A253头颈肿瘤、A549肺癌、A2780卵巢癌、DLD-1结肠癌的细胞毒活性，并与顺铂的细胞毒活性进行比较。考虑到标准偏差，任何细胞系中任何化合物的活性均无显著差异。然而，复合物5对A253头颈部肿瘤表现出最好的IC 50值（6.6 +/-0.2 μ M），而复合物3似乎对A2780卵巢癌最有活性（12.0 +/-0.4 μ M），对DLD-1结肠癌的活性略低（12.4 +/-0.1 μ M）。(C)2009年Elsevier Masson SAS。All rights reserved.
The reaction of 3-methoxyphenylacetic acid, 4-methoxyphenylacetic acid, mesitylthioacetic acid, 2,5-dimethyl-3-furoic acid and 1,4-benzodioxane-6-carboxylic acid with trimethylgallium (1:1) yielded the dimeric complexes [Me2Ga(mu-O2CCH2C6H4-3-OMe)](2) (1), [Me2Ga(mu-O2CCH2C6H4-4-OMe)](2) (2), [Me2Ga(mu-O(2)CCH(2)SMes)](2) (3) (Mes = 2,4,6-Me3C6H2), [Me2Ga{mu-O2C(Fur)}](2) (4) (Fur = 2,5-dimethylfuran) and [Me2Ga{mu-O2C(Bdo)}](2) (5) (Bdo = 1,4-benzodioxane) respectively. The molecular structure of 5 was determined by X-ray diffraction studies. The cytotoxic activity of the gallium(Ill) complexes (1-5) was tested against human tumor cell lines 8505C anaplastic thyroid cancer, A253 head and neck tumor, A549 lung carcinoma, A2780 ovarian cancer, DLD-1 colon carcinoma and compared with that of cisplatin. Taking into account the standard deviation, there is no significant difference in the activity for any of the compounds in any cell line. However, complex 5 presents the best IC50 value against A253 head and neck tumor (6.6 +/- 0.2 mu M), while complex 3 seems to be the most active against A2780 ovarian cancer (12.0 +/- 0.4 mu M) and marginally on DLD-1 colon carcinoma (12.4 +/- 0.1 mu M). (C) 2009 Elsevier Masson SAS. All rights reserved.