| Literature DB >> 20036537 |
Chiao-Ting Yen1, 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.
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(50) values of 1.2 and 1.9 microM, 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 IC(50) values of 6-11 microM against the four tested cancer cell lines. Copyright (c) 2009 Elsevier Ltd. All rights reserved.Entities:
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Year: 2009 PMID： 20036537 PMCID： PMC2831747 DOI： 10.1016/j.bmcl.2009.12.041
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823