Researchers from the Department of Experimental Biology, Faculty of Science, Palacký University Olomouc, contributed to the development of a new synthetic method for the preparation of previously difficult-to-access derivatives of boldine, a natural alkaloid found in the South American boldo tree (Peumus boldus). Using a copper-catalyzed Chan–Lam reaction, the team synthesized a total of 30 novel 9-O-arylated boldine derivatives. The reaction proceeds under mild conditions at room temperature and represents an efficient strategy for expanding the chemical diversity of natural products.
The newly prepared compounds were evaluated in an acute myeloid leukemia (MV4-11) cell model. While boldine itself exhibited only weak activity, most of the new derivatives inhibited cancer cell growth more effectively and displayed low micromolar potency. The study demonstrates that targeted chemical modification of natural products can generate new molecules with promising potential for the future development of anticancer therapeutics.
ACS Omega 2026