The invention addresses
radioresistance in
cancer treatment involving radiotherapy and, in particular, limitations associated with the use of the
drug sulfasalazine. Specifically, it provides a series of compounds for use as radiosensitizers in the treatment of cancers such as glioblastomas which are lethal and inherently resistant to radiotherapy. In one embodiment, the invention provides compounds of general formula (I), their stereoisomers and pharmaceutically acceptable salts for use as radiosensitizers in the treatment of
cancer:wherein ring A is selected from optionally substituted phenyl,
biphenyl and fluorenyl; each X is independently selected from: —C1-6
alkyl (preferably C1-3
alkyl, e.g. —CH3), —O—C1-6
alkyl (preferably —O—C1-3 alkyl, e.g. —OCH3), —S—C1-6 alkyl (preferably —S—C1-3 alkyl, e.g. —SCH3), —OH, —SH, —CO2R1 (where R1 is H or C1-6 alkyl, preferably C1-3 alkyl, e.g. —CH3), —SO2—C1-6 alkyl (preferably —SO2—C1-3 alkyl, e.g. —SO2—CH3), —SO2—NR2R3 (where R2 is H and R3 is optionally substituted phenyl), —NR4R5 (wherein R4 and R5 are independently selected from H, C1-6 alkyl (preferably C1-3 alkyl, e.g. —CH3), and —CO—C1-6 alkyl (preferably —CO—C1-3 alkyl, e.g. —CO—CH3),
halogen (e.g. F, Cl or Br), and optionally substituted tetrazolyl; n is an integer from 0 to 5, preferably 0 to 2, e.g. 1 or 2; and denotes an E or Z
double bond.