Beschreibung:
<jats:title>Abstract</jats:title><jats:p>A variety of new symmetrical and unsymmetrical diketopiperazines have been prepared from free amino acids by using a previously developed microwave‐assisted protocol. This included the successful incorporation of <jats:sc>L</jats:sc>‐pyroglutamic acid as an unusual building block. The diketopiperazines were then thiolated electrophilically to the corresponding bis(methylthio)‐ and epidithiodiketopiperazines. Initial experiments showed a promising activity towards the generation of reactive oxygen species in HeLa cells.</jats:p>