双核镓(III)羧酸配合物的抗癌活性。
Anticancer activity of dinuclear gallium(III) carboxylate complexes.
机构信息
Department of Oral, Maxillofacial and Facial Plastic Surgery, University of Leipzig, Nürnberger Str 57, D-04103 Leipzig, Germany.
出版信息
Eur J Med Chem. 2010 Feb;45(2):519-25. doi: 10.1016/j.ejmech.2009.10.038. Epub 2009 Oct 31.
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 Me(2)Ga(micro-O(2)CCH(2)C(6)H(4)-3-OMe) (1), Me(2)Ga(micro-O(2)CCH(2)C(6)H(4)-4-OMe) (2), Me(2)Ga(micro-O(2)CCH(2)SMes) (3) (Mes=2,4,6-Me(3)C(6)H(2)), Me(2)Ga{micro-O(2)C(Fur)} (4) (Fur=2,5-dimethylfuran) and Me(2)Ga{micro-O(2)C(Bdo)} (5) (Bdo=1,4-benzodioxane) respectively. The molecular structure of 5 was determined by X-ray diffraction studies. The cytotoxic activity of the gallium(III) 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 IC(50) value against A253 head and neck tumor (6.6+/-0.2 microM), while complex 3 seems to be the most active against A2780 ovarian cancer (12.0+/-0.4 microM) and marginally on DLD-1 colon carcinoma (12.4+/-0.1 microM).
3-甲氧基苯乙酸、4-甲氧基苯乙酸、均三甲硫基乙酸、2,5-二甲基-3-呋喃酸和 1,4-苯并二恶烷-6-羧酸与三甲基镓（1:1）反应生成二聚体配合物[Me2Ga(micro-O2CCH2C6H4-3-OMe)]2(1)、[Me2Ga(micro-O2CCH2C6H4-4-OMe)]2(2)、[Me2Ga(micro-O2CCH2SMes)]2(3)（Mes=2,4,6-Me3C6H2）、[Me2Ga{micro-O2CFur)}]2(4)（Fur=2,5-二甲基呋喃）和[Me2Ga{micro-O2CBdo)}]2(5)（Bdo=1,4-苯并二恶烷）。通过 X 射线衍射研究确定了 5 的分子结构。测试了镓(III)配合物(1-5)对人类肿瘤细胞系 8505C 甲状腺癌、A253 头颈部肿瘤、A549 肺癌、A2780 卵巢癌、DLD-1 结肠癌的细胞毒性活性，并与顺铂进行了比较。考虑到标准偏差，任何一种化合物在任何细胞系中的活性都没有显著差异。然而，配合物 5 对 A253 头颈部肿瘤的 IC50 值最低（6.6+/-0.2 microM），而配合物 3 似乎对 A2780 卵巢癌（12.0+/-0.4 microM）和 DLD-1 结肠癌（12.4+/-0.1 microM）具有一定的活性。
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