Design, synthesis, and preliminary biological evaluation of chrysin amino acid derivatives that induce apoptosis and suppress cell migration.

Amino acid derivatives containing chrysin were synthesized for evaluating their anticancer effects. Among them, compound -(7-((5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yl)oxy)heptanoyl)-L-isoleucine () displayed the most potent antiproliferative activity against MGC-803 cells with IC value of 20.0 μM. Preliminary mechanistic studies showed that compound could inhibit the colony formation and migration of MGC-803 cells. Flow cytometry analysis demonstrated that compound mediated cell apoptosis of MGC-803 cells and arrested cell cycle in G2/M-phase. Moreover, treatment in MGC-803 cells downregulated anti-apoptotic protein Bcl-2 and upregulated pro-apoptotic gene Bax in a concentration-dependent manner. Our studies suggest that compound may sever as an effective chemotherapeutic candidate. [Formula: see text].