dimethyl benzoylphenylurea

Dimethyl benzoylphenylurea (BPU), also known as NSC 639829, is an orally active small molecule and a member of the benzoylphenylurea class, which was originally developed for use as insecticides. It was investigated as an antineoplastic agent through a collaboration between Ishihara Sangyo Kaisha and the National Cancer Institute (NCI). BPU acts as a tubulin-interactive agent that binds to the colchicine binding site on tubulin. This binding inhibits tubulin polymerization and disrupts microtubule dynamics, leading to cell cycle arrest in the G2/M phase and subsequent apoptosis. While BPU demonstrated potent preclinical activity across various human tumor xenograft models, its clinical progression was limited by poor and highly variable oral bioavailability and dose-limiting toxicities, including myelosuppression and gastrointestinal effects. Phase I clinical trials were conducted for advanced solid tumors, but development has since been discontinued.

Other names

dimethylamino benzoylphenylureaN,N-dimethylamino benzoylphenylureaN-[4-(5-bromo-2-pyrimidinyloxy)-3-methylphenyl]-N'-(2-dimethylaminobenzoyl)urea