TU-100 (14-methyl-5H-5,12-epiminobenzo[4,5]cyclohepta[1,2-b]naphthalene-6,11,13(12H)-trione) demonstrates remarkable chemotherapeutic capabilities. It acts through a unique mechanism that induces cell death to generate cytotoxicity and simultaneously inhibits both topoisomerase I and II. Its effectiveness can be compared to that of established chemotherapeutic agents like Daunorubicin, while also acting more rapidly. These unique features of TU100 have spurred efforts to develop structurally analogous compounds in pursuit of even more potent bioactive alternatives. TU100 was synthesized by a 1,3-dipolar cycloaddition reaction with 4-hydroxy-N-methylisquinolium iodide and 1,4-naphthoquinone. The analog synthesis will incorporate quinoxaline or its derivatives that have already demonstrated promising chemotherapeutic effects. Synthesizing the hetero naphthoquinones requires a multi-step synthetic process, so quinoxaline/ derivatives intermediates will be prepared first, then the intermediates will be reacted with 4-hydroxy-N-methylisoquinolinum iodide to yield the TU100 analogs. The TU100 analogs will undergo anti-cancer bioassays, with their bioactivity compared to that of TU100.
