merbarone

Merbarone is a small molecule anticancer agent and a nonsedating derivative of thiobarbituric acid. It acts as a catalytic inhibitor of topoisomerase II, blocking the enzyme's ability to mediate DNA cleavage without stabilizing DNA-topoisomerase II covalent complexes. Unlike other topoisomerase II inhibitors such as etoposide, merbarone does not intercalate into DNA or bind in the minor groove but interferes with DNA replication by binding directly to topoisomerase II at a domain potentially shared with other cleavage-enhancing agents. Merbarone has demonstrated cytotoxic and genotoxic effects in preclinical studies and was evaluated in clinical trials for its antineoplastic (anticancer) activity[1][2][3][4][6].

Other names

5-(N-Phenylcarboxamido)-2-thiobarbituric acid5-(N-Phenylcarbamoyl)-2-thiobarbituric acid