Abstract: Therapeutically effective 2,4,5-trisubstituted imidazole compounds are provided. Also provided are methods of preparing the compounds and pharmaceutical compositions comprising the compounds alone or in combination with other agents.

Abstract: Therapeutically effective 2,4,5-trisubstituted imidazole compounds are provided. Also provided are methods of preparing the compounds and pharmaceutical compositions comprising the compounds alone or in combination with other agents.

Abstract: 2-indolyl imidazo[4,5-d]phenanthroline compounds of Formula (I) and methods of using same in the treatment of cancer, in particular, solid cancers and leukemia are provided. Pharmaceutical compositions comprising the compounds are also provided.

Abstract: 2-indolyl imidazo[4,5-d]phenanthroline compounds of Formula I that are capable of intracellular chelation of transition metals and of exerting antiproliferative effects in cancer cells, that are cytostatic and/or cytotoxic, are provided. Compounds of Formula I can also induce apoptosis in cancer cells and are thus capable of exerting a cytotoxic effect on cancer cells. The compounds of Formula I are also capable of selectively inhibiting the proliferation of one or more of prostate cancer cells, colon cancer cells, non-small lung cancer cells and leukemia cells. The compounds of Formula I are also capable of increasing the expression of the zinc-regulated tumour suppressor, KLF4 and thus are useful in inhibiting the proliferation of cancer cells in which KLF4 functions as a tumour-suppressor, including, but not limited to, bladder cancer, cancers of the gastrointestinal tract and various leukemias.