NOVEL FLUORESCENT DERIVATIVES OF POLYAMINES, THEIR METHOD OF PREPARATION AND THEIR APPLICATIONS AS DIAGNOSIS TOOLS IN THE TREATMENT OF CANCEROUS TUMORS
The present invention relates to novel fluorescent derivatives of polyamines having a benzoxadiazole group, their method of preparation and their use as diagnosis tools to allow evidencing of polyamine transport system in cancer cells, and hence to select patients carrying said tumours with a view to adapting their treatment.These derivatives correspond to formula 1:or a pharmaceutically acceptable salt thereof, in which: R1represents one or more NO2groups at position 4 or 6, or a SO2Ph, SO2NMe2, SO2NH2, SO3H group, R2is a hydrogen, a C1-6alkyl, a benzyl, a perfluoroalkyl group, the values of a, b, c can be 2 to 5, independently of each other and represent alkylene chains separating the amino groups, and The values of d and e may independently be 0 or 1.本發明論及新穎之具有一苯并氧雜噁二唑基團的聚胺螢光衍生物、其之製備方法以及其作為診斷工具以允許在癌細胞中聚胺傳遞系統的證明且因此以選擇帶有該等腫瘤的患者目的在於配合其等之治療的用途。這些衍生物對應於化學式1:或其之一藥學上可接受的鹽類,其中:R1代表在位置4及/或6的一或兩個NO2基團、或一SO2Ph、SO2NMe2、SO2NH2、SO3H基團,R2為一氫、一C1-6烷基、一苄基、一全氟烴基基團,A、b、c的值與彼此無關可為2至5且代表分開該等胺基基團的亞烷基鏈,以及d和e的值可獨立地為0或1。
