Synthesis and Cytotoxicity of 4-(2-Adamantyl)phenylalkylamines

What is it about?

Compounds with adamantane core skeletons have been of interest to medicinal chemists since the early1960s. The adamantyl group is present in seven registered therapeutic agents currently in clinical use, and in many other agents in clinical development for the treatment of conditions such as iron overload disease, tuberculosis, malaria and cancer. In many cases, the adamantyl group has been found to increase the drug-like properties of a lead compound without increasing toxicity. We have investigated the antiproliferative activity of the novel 4-(2-adamantyl)arylalkylamines of type 1-4 to elucidate the role of the two benzene rings and the C2-substitution of the adamantane ring in the cytotoxicity of the molecules. Analogues 1-4 were tested against four different tumor cell lines and found to be cytotoxic with low micromolar IC50 values

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