The preparation of 2,6-disubstituted pyridinyl phosphine oxides as novel anti-cancer agents |
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| Authors: | 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 Andrew Kit Wah Chan Paul Bo San Lai Stanton Hon Lung Kok Chor Hing Cheng Albert Sun Chi Chan Johnny Cheuk On Tang |
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| Institution: | 1. Department of Applied Biology and Chemical Technology, Institute of Textiles and Clothing, Hong Kong Polytechnic University, Hong Kong, China;2. BioPharmaNet, Department of Biochemistry and Molecular Biology, The University of Ferrara, Ferrara, Italy;3. Department of Medicine and Therapeutics, Li Ka Shing Medical Sciences Building, Prince of Wales Hospital, The Chinese University of Hong Kong, Hong Kong, China;4. Department of Surgery, Li Ka Shing Medical Sciences Building, Prince of Wales Hospital, The Chinese University of Hong Kong, Hong Kong, China |
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| Abstract: | 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. |
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