Design, syntheses and biological evaluation of natural product aiphanol derivatives and analogues: Discovery of potent anticancer agents.
A recent study investigated the anticancer properties of aiphanol, a natural product found in traditional Chinese medicine. The researchers discovered that aiphanol can inhibit angiogenesis and tumor growth by blocking the VEGF/VEGFRs and COX2 signaling pathways. They designed and synthesized 40 derivatives and analogues of aiphanol, and two of them, 10j and 14c, showed the strongest inhibition of tumor cell growth across various cell lines. These analogues had 80 times greater potency than the original compound. The study also revealed that the presence of a specific substrate at the 7-position of benzo 1,4-dioxane is crucial for the anticancer activity. Molecular docking experiments showed that compound 14c binds tightly to both VEGFR2 and COX2. Overall, compounds 10j and 14c hold promise as potential candidates for future development of anticancer agents.
- Yao L et al (2023).
- Bioorg Med Chem Lett.
- PubMed:
- 37182611