POTENTIAL ANTI-TUMOR TRANSITION METAL COMPLEXES

代表潜在的第三代抗肿瘤药物的新型铂(II)配合物 将制备肿瘤药物并与广泛使用的药物进行比较 顺铂、顺铂(NH3)2Cl2及其第二代类似物。这个 主要目标是找到不显示交叉的新的复合体。 对顺铂耐药的肿瘤的耐药性。载体配体到 用于制备的络合物将包括杂环胺，如 具有自身生物特性的噻唑和咪唑类化合物 活动。喹啉离子具有抗肿瘤作用的链状配体 活性通过柔性链连接到载体配体上 也有待研究。也可以使用可能的嵌入剂来制备 具有栓系配体的配合物。将使用离开小组的变化 以改善络合物的水溶性能。相关复合体 与其他金属如Rh、Ir、Au和Ru一起准备，所有的 进行细胞毒性筛查。复合体的特征将是 光谱分析和X射线衍射法。两人之间的相互作用 将用核碱基、含硫试剂、 DNA和细胞膜。

New complexes of Pt(II) which represent potential third-generation anti- tumor drugs will be prepared and compared to the widely used drug cisplatin, cis-Pt(NH3)2Cl2 and its second-generation analogs. The principal objectives are to find new complexes which do not show cross- resistance in tumors which are resistant to cisplatin. Carrier ligands to be used in preparing the complexes will include heterocyclic amines such as thiazole and imidazole derivatives which have their own biological activities. Tethered ligands in which quinolinium ions with anti-tumor activity are linked to the carrier ligands through flexible chains will also be studied. Possible intercalators may also be used in preparation of complexes with tethered ligands. Variations in leaving groups will be used to improve the aqueous solubilities of the complexes. Related complexes with other metals such as Rh, Ir, Au, and Ru will be prepared and all will be screened for cytotoxicity. Complexes will be characterized by spectroscopic and X-ray diffraction methods. The interactions of the complexes will be studied with nucleobases, sulfur-containing reagents, DNA, and cell membranes.