Total Syntheses and Cytotoxicity Evaluation of Coryaurone A and Representative Analogues

The first total synthesis of coryaurone A, which was originally obtained from Psoralea corylifolia L., was achieved via an efficient route with the longest linear sequence of six steps from the commercially available 6-hydroxy-2H-benzofuran-3-one in 37% overall yield. A series of representative analogues were synthesized from the same starting material in 4-7 steps with overall yields of 27-56%. The cytotoxicities of these compounds against the leukemia cell line HL-60 and the colon cancer cell line SW480 were determined. Among them, compounds 12, 14, 21, and 27 exhibited different levels of cytotoxic activity, which were greater than the positive control cisplatin.