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Total Syntheses and Cytotoxic Evaluations of Cryptolactones A1, A2, B1, B2, and Their Derivatives
Makoto Inai1, Yuki Oguri2, Mitsuyo Horikawa2
1School of Pharmaceutical Sciences, University of Shizuoka.
Chemical & Pharmaceutical Bulletin
|April 3, 2020
Abstract:
The cryptolactones A1, A2, 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.

