Design, synthesis and anti-tumor activity of matrine derivatives as Hsp90 inhibitors.

This study investigates the effects of novel matrine derivatives as heat shock protein 90 (Hsp90) inhibitors on the proliferation, cloning, and migration ability of lung cancer A549 cells along with their mechanisms. In this work, we used matrine as a lead compound with the research objectives of improving its targeting and anti-tumor activity, as well as developing Hsp90 inhibitors with novel structures. We designed and synthesized 21 matrine derivatives based on the C-14 position of matrine.

Design, synthesis and in vitro and in vivo biological evaluation of matrine derivatives as efficient anticancer agents with the characteristics of endoplasmic reticulum stress induction and apoptosis activation.

Natural products have made significant contributions to the prevention and treatment of malignant tumors. However, natural products often suffer from low efficacy and potential toxicity. Therefore, modifying and optimizing lead compounds derived from natural products is a crucial strategy in drug development.