[4][5] As small-molecule, synthetic, DNA minor groove binding alkylating agents, duocarmycins are suitable to target solid tumors.
[6][7] The irreversible alkylation of DNA disrupts the nucleic acid architecture, which eventually leads to tumor cell death.
Analogues of naturally occurring antitumour agents, such as duocarmycins, represent a new class of highly potent antineoplastic compounds.
This research has led to synthetic analogs including adozelesin, bizelesin, and carzelesin which progressed into clinical trials for the treatment of cancer.
Scientists at The Netherlands-based Byondis (formerly Synthon) have combined a unique linkers with duocarmycin derivatives that have a hydroxyl group which is crucial for biological activity.