Plk1 Inhibitors - Isoflavone Study On Sulfone Synthesis Of Analogues Of Styrene

With the gradually recognition of the Polo-like Kinases(PLKs)' biological characteristics, the PLKl inhibitors have become the research emphasis of anti-tumor drugs, and the full-syntheses of new small-molecule PLKl inhibitors have been one of the hottest pharmaceutical fields.It is discovered that benzyl-styrylsulfone derivatives (figure 1) are new compounds with potent anti-tumor activity. 0N01910. Na (Fig 2), one of its candidates, competed for the substrate binding site of the PLKl, can result in mitotic arrest of tumor cells characterized by spindle abnormalities leading to their apoptosis, and demonstrate potent anti-tumor activity both in vitro and in vivo. Besides, it did not exhibit any toxicity nor drug-tolerance, and was a promising compound. Thus, we intended to place 0N01910.Na as leading compound, reserve its benzyl-styrylsulfone structure, synthesis a series of derivatives and carry out the anti-tumor assay.Recently, reports on the anti-tumor activities of the isoflavonoid derivatives have been increasing, these compounds are potent anti-tumor agents, and they are cheap, simple to synthesis, and able to be modified,. So, they are valuable compounds.This paper is going to associate the structure core of isoflavonoid and benzyl-styrylsulfone selectivily to get the target derivatives, i. e. isoflavonoid -styrylsulfone. We will also alter the substitutes to synthesis compounds without patent protecting as 0N01910. Na to be the leading compound. We will carry out the anti-tumor activity determination in order to discover new small-molecule anti-tumor compounds, and confirm their structures.