PYRROLO [2,1-C][1, 4] BENZODIAZEPINE-GLYCOSIDE PRODRUGS USEFUL AS A SELECTIVE ANTI TUMOR AGENT

摘要

The present invention provides novel pyrrolo[2,1-c][1, 4]benzodiazepine- glycoside prodrug of general formula (1a-b), useful as selective anticancer agents. The present invention also provides a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine-glycoside prodrugs of general formula (1a-b). This invention also provides activation of these produgs by E.coli ß galactosidase and envisaged that these molecules are toxic to human cancer cell lines in the presence of the enzyme E.coli ß -galactosidase. The prodrugs (1a and 1b) were also found to be toxic to human cancer HepG2 cells even in the absence of the E.coli ß-galactosidase. The toxic effect of the molecules when activated was similar to that of the parent molecules (6a and 6b), respectively.