Syntheses of Metal Complexes for Diagnosis and Imaging of Tumor Tissue

水溶性卟啉衍生物在肿瘤或癌组织中的选择性富集，为光化学方法辅助早期癌症的诊断和治疗提供了工具。然而，该方法的应用仅限于浅表肿瘤的诊断。因此，从组织表面探测深部肿瘤的位置并对其进行三维成像，需要更多的高分辨率的化学证据。第一种方法是将放射性元素掺入化学物质中，选择性地结合到肿瘤组织上。用紫外光照射卟啉和碘的混合物进行次卟啉的碘化反应，用放射性碘高度稀释的碘制备特殊卟啉是可行的。荧光法和照相法都可用于检测组织深部的肿瘤。第二个化学证据是使用了哺乳动物组织中没有的氟化染料。组织<19>中氟化产物的1H-NMR谱可以高灵敏度地观察到。对于<19>全氟烷基取代的卟啉的顺磁性金属络合物，也可以测量13 F-共振的各向同性位移。水溶性的含氟卟啉及其金属配合物通过新的合成方法很容易得到。含氟染料及其金属配合物是通过新的合成方法容易获得的。氟化染料和络合物使我们能够通过光化学方法、电子自旋共振和NMR光谱来检测肿瘤位置并确定其大小。

Selective accumulation of water-soluble porphyrin derivatives to tumor or cancer tissue have provided tool for diagnosis and therapy of earlier cancer with aid of photochemical method. However, application of this method is limited to diagnosis of superfacial tumor. Therefore, more elablrate chemical proves are required to detect the position of deep tumor from tissue surface and to make its three dimensional imaging. The first approach is incorporation of radioactive element in chemical prove selectively bound to the tumor tissue. Iodination of deuteroporphyrin was carried our by UV-irradiation of the mixture of porphyrin and iodine.Present method is available to prepare particular porphyrin by using iodine highly diluted with radiocative one. Both fluorescence and photographic measurements can be applied to detect tumor in the deep place of tissues.The second chemical prove is use of fluorinated dyes which are not found in mammalian tissues. ^<19>F-NMR spectra of the fluorinated proves in tissues are observable in high sensitivity. Isotropic shifts of ^<19>F-resonance are also measurable for the paramagnetic metal complexes of perfluoroalkyl- substituted porphyrins. Water soluble fluorinated porphyrins and their metal complexes are readily obtained by new synthetic method. Fluorinated dyes and their metal complexes are readily obtained by new synthetic method. Fluorinated dyes and complexes enable us to detect of tumor location and to define its size by photochemical method, electron spin resonance, and NMR spectroscopy.