toyaburgine

Toyaburgine is a synthetic N-biphenyl-dihydroisoquinoline inspired by naturally occurring N,C-coupled naphthylisoquinoline alkaloids. It is being developed as a potent anticancer agent specifically targeting pancreatic cancer, a malignancy characterized by high chemoresistance and a nutrient-deprived tumor microenvironment. Toyaburgine exhibits strong "antiausterity" activity, meaning it effectively inhibits the viability of cancer cells under stressful, nutrient-poor conditions with low nanomolar potency. Mechanistically, the compound disrupts the PI3K/Akt/mTOR signaling pathway, which is critical for the survival of pancreatic cancer cells in stressful environments. Preclinical studies in MIA PaCa-2 models have demonstrated its ability to inhibit cell migration, colony formation, and spheroid growth. In vivo, toyaburgine has shown significant tumor suppression in both subcutaneous and orthotopic xenograft models, both as a monotherapy and in combination with gemcitabine, while also demonstrating potential in reducing cancer-associated cachexia.

Other names

toyaburgineN-biphenyl-dihydroisoquinoline