Magnolol-Coumarin-Phenylbutyric acid Conjugates: An Anticancer Prodrug via multiple targets

Abstract

We present here, the design and synthesis of a phenylbutyric acid-magnolol-coumarin conjugates (5). Compound 5 is a multifunctional molecule composed of magnolol, coumarin, phenylbutyric acid as model active drugs via ester. Upon entering tumor cells, ester bond cleavage occurs as well as active drug magnolol, coumarin and phenylbutyric acid release to attack cancer cells. In vitro anti-proliferation experiments showed that the inhibitory activity of compound 5 against HepG2, MCF-7, A431 and A549 cells was significantly higher than that of its single parent compound. Moreover, compound 5 had a long-term effect. Due to fluorescence of compound 5, it can serve as a fluorescence imaging agent and its uptake can be monitored. Compound 5 may provide a reference for the design of new derivatives of magnolol.