The preparation of 2,6-disubstituted pyridinyl phosphine oxides as novel anti-cancer agents

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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.

Graphical abstract

The preparation of 2,6-disubstituted pyridinyl phosphine oxides and their antitumor properties were reported.

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Acknowledgments

We acknowledge a donation fund from Mr. KC Lo to Dr JCO Tang for the establishment of Lo Ka Chung Centre for Natural Anti-cancer Drug Development (Laboratory B) and a Niche area grant offered by the Hong Kong Polytechnic University to Dr KH Lam and Dr. JCO Tang (BB8T, HK$100,000). Professor R Gambari is sponsored by AIRC (Italian Association for Cancer Research). Dr. CH Chui is supported by the Research Assistant Professorship offered by Professor GYM Cheng (Haematology Research Funding) and

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