| Abstract
| - Iron deprivation has been previously proven to be a promising strategy in treating tumor cells. Aseries of cis,cis-1,3,5-triaminocyclohexane N-pyridyl derivatives as iron-depleting antitumor agentswere prepared. Cytotoxic activity of these derivatives was evaluated in the HeLa cancer cell line.Among the tested derivatives, N-ethyl-N,N‘,N”-tris(2-pyridylmethyl)-cis,cis-1,3,5-triaminocyclohexane (17) exhibited potent cytotoxicity against this cancer cell line. On the basis of the structureof 17, a bifunctional iron chelator 24 was designed and prepared. Bifunctional agent 24 possessinga maleimide linker that is functional for conjugation to thiolated monoclonal antibodies is apromising lead compound for development of antitumor conjugates for antibody-targeted therapies.
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