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Antitumor agents. 271: Total synthesis and evaluation of brazilein and analogs as anti-inflammatory and cytotoxic agents
Chiao-Ting Yen; Kyoko Nakagawa-Goto; Tsong-Long Hwang; Pei-Chi Wu; Susan L. Morris-Natschke; Wan-Chun Lai; Kenneth F. Bastow; Fang-Rong Chang; Yang-Chang Wu; Kuo-Hsiung Lee (Profiled Authors: Susan L Morris-Natschke; Kenneth F Bastow; Kuo-Hsiung Lee; Kyoko Nakagawa-Goto)
Bioorganic and Medicinal Chemistry Letters. 2010;20(3):1037-1039.Abstract
The first total synthesis of the naturally occurring tetracyclic homoisoflavonoid brazilein (1) and 14 new analogs (1a-n) is reported. Target compounds and intermediates were assayed for anti-inflammatory effects on superoxide anion generation and elastase release by human neutrophils in response to fMLP/CB, and for cytotoxic activity against nasopharyngeal (KB), vincristine-resistant nasopharyngeal (KBvin), lung (A549) and prostate (DU-145) human cancer cell lines. The most active compound 1b showed potent effects on superoxide anion generation and elastase release with IC
PMID: 20036537 PMCID: PMC2831747
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