Bioorganic & Medicinal Chemistry Letters 2012-06-15

Design and synthesis of gambogic acid analogs as potent cytotoxic and anti-inflammatory agents

Chiao-Ting Yen, Kyoko Nakagawa-Goto, Tsong-Long Hwang, Susan L. Morris-Natschke, Kenneth F. Bastow, Yang-Chang Wu, Kuo-Hsiung Lee

Index: Bioorg. Med. Chem. Lett. 22(12) , 4018-22, (2012)

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Abstract

Two pyranoxanthones (16 and 20) showed the greatest activity against the KBvin multidrug resistant (MDR) cell line with IC50 values of 0.9 and 0.8μg/mL, respectively. An angular 3-methyl-3-prenyl pyranoxanthone (17) selectively inhibited elastase release with 200 times more potency than PMSF, the positive control.