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Dendrocandins are characteristic chemical structures of D. officinale and have strong physiological bioactivities. In this study, a dendrocandin analogue (1) has been prepared by total synthesis (9 steps, 12.6% overall yield) in which coupling reaction and Wittig reaction as the key steps. Compound 1 was also evaluated for its anticancer activity in vitro against six human cancer cells (MCF-7, A549, A431, SW480, HepG-2 and HL-60) using MTT assays. Compound  1  showed potent cytotoxicity, with the IC50 value 16.27 ± 0.26 µM. The expression levels of apoptotic proteins indicated that compound  1  can up-regulate the expression of apoptotic proteins, leading to apoptosis. This compound suggested that it’s potential as anticancer agent for further development.

Synthesis and in vitro biological evaluation of novel dendrocandin analogue as potential anti-tumor agent