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Paper | Special issue | Vol 30, No. 2, 1990, pp.993-1008
Published online, 1st January, 1970
DOI: 10.3987/COM-89-S101
Structure-Activity Relationships of Pseudoguaianolides Isolated from Gaillardia pulchella and Their Derivatives

Kenzo Harimaya and Seiichi Inayama*

*Pharmaceutical Institute, School of Medicine, Keio University, Shinanomachi 35, Shinjuku, Tokyo 160-0016, Japan

Abstract

Three new pseudoguaianolides, 4-epipulchellin (1), 4-epineopulchellin (2) and pulchelloid D (3), were isolated from Gaillardia pulchella together with other eleven pseudoguaianolides and three guaianolides. Fifteen natural sesquiterpene lactones and their thirty one derivatives were tested for cytotoxic activity against KB cell line. Among them, twenty seven compounds were shown to be active (ED50 < 4 μg/ml). The structure-activity relationships of these sesquiterpene lactones are discussed.