Design of DNA-cleaving and -crosslinking agents based on NFκB and HMGA proteins aiming at the application to cancer therapy

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Recently, NFκB and HMGA proteins attract the interest because of their relation to carcinogenesis and tumor invasion. The present study aimed at design and synthesis of DNA-cleaving/crosslinking molecules based on the NFκB and HMGA proteins.We first synthesized a novel artificial ligand comprising a dimethylaminopyridine and histidines. This ligand formed ferrous complex to generate oxygen radical, cleaving DNA. In the present study, we are successful to prepare a new dimethylaminopyridine/histidine based ligand equipped with a chloroalkyl linker that could bind a SH group of various proteins in situ. This would enable us to cleave DNA sequences that NFκB and HMGA proteins recognize.