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

Author information

Keywords: cryptolactones, asymmetric synthesis, cytotoxicity

JOURNAL FREE ACCESS FULL-TEXT HTML

2020 Volume 68 Issue 4 Pages 380-383

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

Details

Abstract

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.

Graphical Abstract Fullsize Image

Corresponding author

Register with J-STAGE for free!