The preparation of 2,6-disubstituted pyridinyl phosphine oxides as novel anti-cancer agents
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- 作者：Kim Hung Lam ; Roberto Gambari ; Marcus Chun Wah Yuen ; Chi Wai Kan ; Penni Chan ; Lijin Xu ; Weijun Tang ; Chung Hin Chui ; Gregory Yin Ming Cheng ; Raymond Siu Ming Wong ; Fung Yi Lau ; Cindy Sze Wai Tong ; And
- 关键词：Pyridinyl phosphine oxides ; Antitumor ; MDAMB-231 breast cancer ; SKHep-1 hepatoma cell lines
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：15 April 2009
- 年：2009
- 卷：19
- 期：8
- 页码：2266-2269
- 全文大小：341 K
文摘
A series of 2,6-dimethoxylpyridinyl phosphine oxides have been synthesized and examined for their antitumor activity. 2,6-Dimethoxy-3-phenyl-4-diphenylphosphinoylpyridine 2 has been employed as the lead compound for this study. We found out that the presence of phosphine oxide on the 2,6-dimethoxylpyridine ring is important for the antitumor activity; the presence of bromine on this core leads to a further enhancement of its antitumor activity. This is the first reported work on the antitumor activity of the 2,6-dimethoxy-3,5-dibromopyridinyl phosphine oxide 5b towards MDAMB-231 breast cancer and SKHep-1 hepatoma cell lines.