1215097-61-2Relevant academic research and scientific papers
Antitumor agents. 271: Total synthesis and evaluation of brazilein and analogs as anti-inflammatory and cytotoxic agents
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
body text, p. 1037 - 1039 (2010/06/14)
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 IC50 values of 1.2 and 1.9 μM, respectively, and was 65 times more potent than phenylmethylsulfonyl fluoride (PMSF), the positive control, in the latter assay. Additionally, 1b exhibited broad spectrum in vitro anticancer activity with IC50 values of 6-11 μM against the four tested cancer cell lines.
