USE OF EMICORONS AS SELECTIVE INDUCERS OF DAMAGE TO THE TELOMERE DNA

摘要

The hydrosoluble emicoron derivatives of the general formula (I) are particularly effective as inducers of selective telomere and non- telomere DNA damage in tumour and transformed cells. The damage is measured as the ability to cause a number of TIF foci in transformed cells that is equal to or higher than 4 at a 0.1 uM dose of the compound of the formula (I). Such emicoron derivatives can be used in a kit together with other known anti-tumour drugs, such as, for example, topoisomerase I inhibitors, for the combined, simultaneous, delayed or sequential administration. The emicoron compounds of the formula (I) are particularly useful in the therapy of tumours that do not express p53 protein or express an inactive p53 protein and of tumours that maintain telomeres by mechanisms different from telomere maintenance by telomerase, and in the removal of cancer stem cells. Also, the method for the preparation of emicoron compounds of the formula (I), which envisages the use of intermediates such as the Ν,Ν'-bis [2-(1-piperidino)-ethyl] - 1-(1-piperidinyl)-7- [3-(1-piperidino)- butynyl]-perylene-3,4;9,10-tetracarboxyl diimide, is described.