Antitumor agents. 271: Total synthesis and evaluation of brazilein and analogs as anti-inflammatory and cytotoxic agents

CT Yen, K Nakagawa-Goto, TL Hwang, PC Wu…

Index: Yen, Chiao-Ting; Nakagawa-Goto, Kyoko; Hwang, Tsong-Long; Wu, Pei-Chi; Morris-Natschke, Susan L.; Lai, Wan-Chun; Bastow, Kenneth F.; Chang, Fang-Rong; Wu, Yang-Chang; Lee, Kuo-Hsiung Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 3 p. 1037 - 1039

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Citation Number: 39

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 ...