Biological Evaluation of a Potential Anticancer Agent Methyl N -[5-(3'-Iodobenzoyl)-1 H -Benzimidazol-2-yl]Carbamate

Resistance of cancer to chemo- and radiotherapy remains a major clinical problem. This study contributes to the ongoing search for agents that can bypass this resistance by developing a novel antimitotic theranostic. Methyl -[5-(3'-iodobenzoyl)-1 -benzimidazol-2-yl]carbamates and were synthesized from a common precursor or its 3'-stannylated derivative. The cytotoxicity of compound was evaluated in several neuroblastoma and glioblastoma cell lines and in the NCI 60-cell assay. Biodistribution was conducted in mice after oral administration of compound to determine tissue and brain uptake. Lethal concentrations (LC s) of compound in neuroblastoma and glioblastoma are >15 × lower compared with compound , a drug currently tested in clinical studies in pediatric and adult brain tumors. Growth inhibition concentrations (GI ) are in the nanomolar range in 60 cancer cell lines. When compound is combined with a 4-Gy dose of radiation,