Design, synthesis and in vitro cytotoxicity study of benzodiazepine-mustard conjugates as potential brain anticancer agents

摘要: Abstract The combination of two pharmacological entities in a single compound has been utilized as promising drug design strategy for site-specificity. So nitrogen mustard agents were synthesized by conjugating with the benzodiazepine nucleus hope to obtain central nervous system (CNS) antitumor agents. part is aimed serve CNS active carrier enabling alkylating moiety cross BBB altering its physicochemical properties. Structures all compounds confirmed IR, NMR ( 1 H & 13 C), mass spectral and elemental studies. benzodiazepine-mustard conjugates are oily at room temperature quite stable when stored refrigerator 2 months. Both evaluated NBP activity against chlorambucil, proved be markedly subjected vitro biological evaluation using an MTT colorimetric assay four human cancer cell lines (A-549, COLO 205, U-87 MG IMR-32). ADME studies also analyzed Qikprop 2.5 tools Schodinger software which further indicates that both can potential candidates treatment brain tumor.