Structure-activity relationship and mechanistic study on guggulsterone derivatives; Discovery of new anti-pancreatic cancer candidate

Author: Kohyama, A., Kim, M.J., Yokoyama, R., Sun, S., Omar, A.M., Phan, N.D., Meselhy, M.R., Tsuge, K., Awale, S. and Matsuya, Y

Bioorganic & Medicinal Chemistry, 2021


This study focused on screening 14 guggulsterone derivatives (GSDs) for developing new-generation treatments against pancreatic cancer. The CytoSMART Lux2 was used to observe morphological changes PANC-1 cells after treatment with GSD-11, which was the most active treatment. Taking all results together, GSD-11 seems to be a promising compound for treatment of pancreatic cancer, as it has most potent activity, inhibits migration of cancer cells and inhibits colony formation.