School of Chemistry and Chemical Engineering, Lanzhou Jiaotong University, Lanzhou Gansu 730070, People's Republic of China.
J Nat Prod. 2022 Jun 24;85(6):1634-1640. doi: 10.1021/acs.jnatprod.2c00345. Epub 2022 Jun 7.
The first total synthesis of coryaurone A, which was originally obtained from L, was achieved via an efficient route with the longest linear sequence of six steps from the commercially available 6-hydroxy-2-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 , , , and exhibited different levels of cytotoxic activity, which were greater than the positive control cisplatin.
首次实现了源于 L 的角鲨烯 A 的全合成，该合成采用了一种高效的路线，从商业可得的 6-羟基-2-苯并呋喃-3-酮出发，经最长的六步线性序列，以 37%的总收率得到目标产物。以相同的起始原料，经 4-7 步反应，可合成一系列具有代表性的类似物，总收率为 27-56%。测试了这些化合物对白血病细胞系 HL-60 和结肠癌细胞系 SW480 的细胞毒性。其中，化合物 、 、 、 和 表现出不同程度的细胞毒性活性，优于阳性对照顺铂。
