Li Qingshan, da Silva M Fátima C Guedes, Pombeiro Armando J L
Centro de Química Estrutural, Complexo I, Instituto Superior Técnico, Av. Rovisco Pais, 1049-001 Lisbon, Portugal.
Chemistry. 2004 Mar 19;10(6):1456-62. doi: 10.1002/chem.200305266.
A series of diorganotin(IV) and dichlorotin(IV) derivatives of 4-X-benzohydroxamic acids, [HL(1) (X = Cl) or HL(2) (X = OCH(3))] formulated as [R(2)SnL(2)] (R = Me, Et, nBu, Ph or Cl; L = L(1) or L(2)), along with their corresponding mixed-ligand complexes [R(2)Sn(L(1))(L(2))] have been prepared and characterized by FT-IR, (1)H, (13)C, and (119)Sn NMR spectroscopy, mass spectrometry, elemental analysis, and melting points. In addition, single-crystal X-ray diffraction analyses were carried out for [Me(2)SnL(2)] (L = L(1) or L(2)), which show coordination structures intermediate between distorted octahedra and bicapped tetrahedra. The hydroxamate ligands are asymmetrically coordinated by the oxygen atoms, the carbonyl oxygen atom is further away from the metal center than the other oxygen atom. The complexes are stable monomeric species; most of them are soluble not only in chlorohydrocarbon solvents, but also in alcohols and hydroalcoholic solutions. In polar solvents, the mixed-ligand complexes gradually decompose into the corresponding single-ligand complex couples. The complexes exhibit in vitro antitumor activities (against a series of human tumor cell lines) which, in some cases, are identical to, or even higher than, that of cisplatin. For the dialkyltin complexes, the activity increases with the length of the carbon chain of the alkyl ligand and is higher in the case of the chloro-substituted benzohydroxamato ligand. The [nBu(2)Sn(L(1))(2)] complex displays a high in vivo activity against H22 liver and BGC-823 gastric tumors, and has a relatively low toxicity.
一系列4-X-苯甲羟肟酸的二有机锡（IV）和二氯锡（IV）衍生物，[HL(1)（X = Cl）或HL(2)（X = OCH(3)）]，其化学式为[R(2)SnL(2)]（R = 甲基、乙基、正丁基、苯基或氯；L = L(1)或L(2)），以及它们相应的混合配体配合物[R(2)Sn(L(1))(L(2))]已被制备出来，并通过傅里叶变换红外光谱、氢谱、碳谱和锡-119核磁共振光谱、质谱、元素分析和熔点进行了表征。此外，对[Me(2)SnL(2)]（L = L(1)或L(2)）进行了单晶X射线衍射分析，结果表明其配位结构介于扭曲八面体和双帽四面体之间。羟肟酸配体通过氧原子不对称配位，羰基氧原子比另一个氧原子离金属中心更远。这些配合物是稳定的单体物种；它们中的大多数不仅可溶于氯代烃溶剂，还可溶于醇类和水醇溶液。在极性溶剂中，混合配体配合物会逐渐分解为相应的单配体配合物对。这些配合物表现出体外抗肿瘤活性（针对一系列人类肿瘤细胞系），在某些情况下，其活性与顺铂相同，甚至更高。对于二烷基锡配合物，活性随着烷基配体碳链长度的增加而增加，并且在氯取代的苯甲羟肟酸配体的情况下更高。[正丁基(2)Sn(L(1))(2)]配合物对H22肝癌和BGC-823胃癌显示出高体内活性，并且毒性相对较低。
