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Evaluating Itraconazole Analogues And Translesion Synthesis Inhibitors As Anti-Cancer Agents, Kelly Allison Chan

Honors Scholar Theses

My projects were to evaluate itraconazole (ITZ) analogues as anti-cancer hedgehog (Hh) and angiogenesis inhibitors, and translesion synthesis (TLS) inhibitors as anti-cancer agents. Itraconazole (ITZ) is a clinically effective triazole antifungal agent that has also been identified for its anti-cancer properties. As reported in the current literature, ITZ inhibits Gli1 transcription of the Hedgehog (Hh) signaling pathway and angiogenesis. However, the triazole moiety of ITZ has a detrimental side effect of inhibiting cytochrome P450 3A4 enzymes (CYP3A4). Thus, we have removed the triazole from the ITZ scaffold and develop a new series of ITZ analogues called des-triazole ITZ analogues. The …