硫代酰胺配体的新型有机锡（IV）配合物的生物学研究。

Biological studies of new organotin(IV) complexes of thioamide ligands.

作者信息

Xanthopoulou Marianna N, Hadjikakou Sotiris K, Hadjiliadis Nick, Milaeva Elena R, Gracheva Julia A, Tyurin Vladimir Yu, Kourkoumelis Nikolaos, Christoforidis Kostantinos C, Metsios Apostolos K, Karkabounas Spyros, Charalabopoulos Konstantinos

机构信息

Inorganic and Analytical Chemistry, Department of Chemistry, University of Ioannina, 45110 Ioannina, Greece.

出版信息

Eur J Med Chem. 2008 Feb;43(2):327-35. doi: 10.1016/j.ejmech.2007.03.028. Epub 2007 Apr 10.

DOI:10.1016/j.ejmech.2007.03.028

PMID:17509733

Abstract

New organotin(IV) complexes with heterocyclic thioamides 2-mercapto-benzothiazole (Hmbzt), 5-chloro-2-mercapto-benzothiazole (Hcmbzt) and 2-mercapto-benzoxazole (Hmbzo) of formulae [(C(6)H(5))(3)Sn(mbzt)] (1), [(C(6)H(5))(3)Sn(cmbzt)] (3) and [(C(6)H(5))(2)Sn(cmbzt)(2)] (4), together with the already known [(C(6)H(5))(3)Sn(mbzo)] (2), [(n-C(4)H(9))(2)Sn(cmbzt)(2)] (5) and [(CH(3))(2)Sn(cmbzt)(2)] (6) were used to study their influence on the peroxidation of oleic acid. The influence of complexes (3)-(6) upon peroxidation of oleic acid showed that the formation of reactive radicals caused the initiation of the chain radical oxidation of the substrate. The influence of complexes (1)-(6) upon the catalytic peroxidation of linoleic acid by the enzyme lipoxygenase (LOX) was also studied and compared to those of cisplatin. Compounds (1)-(6) were finally tested for in vitro cytotoxicity against leiomyosarcoma cells.

摘要

新型有机锡（IV）与杂环硫代酰胺2-巯基苯并噻唑（Hmbzt）、5-氯-2-巯基苯并噻唑（Hcmbzt）和2-巯基苯并恶唑（Hmbzo）形成的配合物，其化学式分别为[(C(6)H(5))(3)Sn(mbzt)] （1）、[(C(6)H(5))(3)Sn(cmbzt)] （3）和[(C(6)H(5))(2)Sn(cmbzt)(2)] （4），连同已知的[(C(6)H(5))(3)Sn(mbzo)] （2）、[(n-C(4)H(9))(2)Sn(cmbzt)(2)] （5）和[(CH(3))(2)Sn(cmbzt)(2)] （6），被用于研究它们对油酸过氧化的影响。配合物（3）-（6）对油酸过氧化的影响表明，活性自由基的形成引发了底物的链自由基氧化。还研究了配合物（1）-（6）对脂氧合酶（LOX）催化亚油酸过氧化的影响，并与顺铂的影响进行了比较。最后测试了化合物（1）-（6）对平滑肌肉瘤细胞的体外细胞毒性。