Total Syntheses and Cytotoxic Evaluations of Cryptolactones A1, A2, B1, B2, and Their Derivatives

Makoto Inai; Yuki Oguri; Mitsuyo Horikawa; Hiroto Kaku; Shinya Suzuki; Kei Kitamura; Tetsuto Tsunoda

doi:10.1248/cpb.c19-01114

Regular Articles

Total Syntheses and Cytotoxic Evaluations of Cryptolactones A₁, A₂, B₁, B₂, and Their Derivatives

Makoto Inai, Yuki Oguri, Mitsuyo Horikawa, Hiroto Kaku , Shinya Suzuki, Kei Kitamura, Tetsuto Tsunoda

著者情報

キーワード: cryptolactones, asymmetric synthesis, cytotoxicity

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2020 年 68 巻 4 号 p. 380-383

DOI https://doi.org/10.1248/cpb.c19-01114

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抄録

The cryptolactones A₁, A_2, B₁, and B₂ isolated from a Cryptomyzus sp. aphid were synthesized via the Mukaiyama aldol reaction and olefin metathesis. Their antipodes and derivatives were also synthesized by the same strategy to investigate structure–activity relationships. These compounds exhibited cytotoxic activity against human promyelocytic leukemia HL-60 cells with IC₅₀ values of 2.1–42 µM.

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