Potential CNS antitumor agents VI: aziridinylbenzoquinones III

Abstract

Thirty-one aziridinylbenzoquinones were compared against five murine tumor models in vivo. Two intracerebral (ependymoblastoma and L-1210 leukemia) and three intraperitoneal (P-388 and L-1210 leukemia and B16 melanoma) systems were utilized. Excellent activity was observed for many compounds. Multiple long-term survivors were produced in the ependymoblastoma, P-388, and intraperitoneal L-1210 systems. Diethyl 2,5-bis(1-aziridinyl)-3,6-dioxo-1,4-cyclohexadiene-1,4-dicarbamate demonstrated superior activity in all five test systems. This compound also was reproducibly active against two colon tumors, a mammary tumor, and the intracerebrally implanted P-388 leukemia model.