Hypocretenolides: collective total syntheses and activities toward metastatic colon cancer
Bolin Chen1, Xijing Zhang1, Yufen Yang2
1State Key Laboratory of Medicinal Chemical Biology, Frontiers Science Center for New Organic Matter, Nankai University 94 Weijin Road Tianjin 300071 China 017095@nankai.edu.cn lwang@nankai.edu.cn yuechen@nankai.edu.cn.
Abstract:
A concise and collective synthetic route to hypocretenolides was developed for the first time. This route features one-pot addition-alkylation and intramolecular 1,3-dipolar cycloaddition to efficiently assemble the 5/7/6 ring system. Our syntheses enabled multigram preparation of hypocretenolide which facilitated further biological evaluation. Preliminary CCK-8 cytotoxic results of hypocretenolide indicated its IC50 values within 1 μM against 4 colon cancer cell lines. Wound healing and transwell assays suggested the promising inhibitory activities of hypocretenolide toward the migratory capabilities of colon cancer cells in vitro. The animal results confirmed that hypocretenolide can inhibit metastasis of colon cancer cells.
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