Cyclams are macrocyclic polyamines which medical interest was fueled by the therapeutic potential of a bicyclam derivative in HIV infection, inflammatory diseases, cancer and stem-cell mobilization. Taking advantage of the biocompatibility, the high metal chelation stability constants and the possibility of N-functionalization of the cyclam backbone, a variety of compounds have been explored in a wide range of medicinal applications. The use of cyclams and cyclam-based complexes as antimicrobial and antitumoral agents has been described in recent years. In particular, trans-disubstituted cyclam salts revealed to be active antibacterial agents against both Gram-positive and Gram-negative bacteria.[3,4]
In the field of anticancer applications, several attempts are being made, mostly with CuII complexes, envisaging their use as 64/67Cu radionuclides. Recently, we found that trans-disubstituted cyclam derivatives and their CuII and FeIII complexes display relevant antitumoral activity against HeLa cancer cell lines. To the best of our knowledge, this is the first report on an iron-cyclam compound tested as anticancer agent.
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