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Eight new stigmasterol derivatives possessing 1,2,3-triazoles moiety were synthesized by a 1,3-dipolar cycloaddition reaction. All the compounds were characterized by IR, NMR, and HR-MS. In addition, human cervical cancer cells (HeLa), human gastric cancer cells (HGC-27), and human renal epithelial cells (HEK-293T) were selected to study the antitumor activity of the synthesized compounds. The results demonstrated that compounds 3c and 3d exhibited better inhibitory activity against the tested tumor cell lines. The IC50 value of the inhibitory activity on HeLa was 52.3 μmol·L–1 and 31.4 μmol·L–1, and 40.6 μmol·L–1 and 44.6 μmol·L–1 for HGC-27, respectively. [ABSTRACT FROM AUTHOR]

An efficient Ir(III)-catalyzed decarbonylative annulation of salicylaldehydes with cyclohexane-1,3-diones has been achieved via the in situ generated iodonium ylides. The reaction proceeds smoothly under mild and operationally simple conditions, affording a variety of benzofuran derivatives in moderate to high yields with good functional group tolerance. Moreover, the large-scale synthesis and further modification of the products highlight the utility of this protocol. [ABSTRACT FROM AUTHOR]