The synthesis and characterization of two hybrid N-methylated carbazole derivatives containing a thiazolyl or a thienyl ring is reported. The thiazolyl derivative has been also characterised by X-ray diffraction analysis. The study of its reactivity in front of [MCl₂(dmso)₂] (M = Pd or Pt) or Na₂[PdCl₄] in methanol has allowed us to isolate and characterize its complexes. However, for the thienyl analogue, the formation of any Pd(II) or Pt(II) complex was not detected, indicating that it is less prone to bind to the M(II) ions than its thiazolyl analogue. Density Functional Theory (DFT) and Time-Dependent Density Functional Theory (TD-DFT) calculations have also been carried out in order to rationalize the influence of the nature of the thiazolyl or thienyl group on the electronic delocalization. Molecular mechanics calculations show that the free rotation of the thiazolyl in relation to the carbazole requires a greater energy income than for its thienyl analogue. Studies of the cytotoxic activity of the new compounds on colon (HCT116) and breast (MDA-MB231 and MCF7) cancer cell lines show that the thiazolyl carbazole ligand and its Pt(II) complex are the most active agents of the series and in the MCF7 line their potency is higher than that of cisplatin. In the non-tumoral human skin fibroblast BJ cell line, all the compounds were less toxic than cisplatin. Their potential ability to modify the electrophoretic mobility of pBluescript SK⁺ plasmid DNA and to act as inhibitors of Topoisomerases I and IIα or cathepsin B has also been investigated.

报道了两种含有噻唑基或噻吩基环的杂化N-甲基化咔唑衍生物的合成和表征。噻唑基衍生物也已经通过X射线衍射分析表征。在[MCl ₂（dmso）₂ ]（M = Pd或Pt）或Na ₂ [PdCl ₄甲醇中的]使我们能够分离和表征其络合物。但是，对于噻吩基类似物，未检测到任何Pd（II）或Pt（II）配合物的形成，这表明与噻唑基类似物相比，它更不易于与M（II）离子结合。为了合理化噻唑基或噻吩基的性质对电子离域的影响，还进行了密度泛函理论（DFT）和时变密度泛函理论（TD-DFT）计算。分子力学计算表明，噻唑基相对于咔唑的自由旋转比噻吩基类似物需要更多的能量收入。新化合物对结肠癌细胞（HCT116）和乳腺癌细胞（MDA-MB231和MCF7）的细胞毒活性研究表明，噻唑基咔唑配体及其Pt（II）络合物是该系列中最活跃的药物， MCF7品系的效力高于顺铂。在非肿瘤性人类皮肤成纤维细胞BJ细胞系中，所有化合物的毒性均低于顺铂。它们潜在的修饰pBluescript SK电泳迁移率的能力^{还研究了+}质粒DNA并充当拓扑异构酶I和IIα或组织蛋白酶B的抑制剂。