We describe the synthesis of a group of (2-(substituted benzylsulfonyl) ethyl) substituted benzenes which induce apoptotic death of a wide variety of human tumor cell lines at sub-nanomolar concentrations while exhibiting relatively low toxicity to normal human cells. Our studies show that the cytoxic activity of the arylethyl benzyl sulfones is totally dependent on the nature and position of the substituents on the two aromatic rings. The structure function studies show that a molecule with a benzyl moiety having 3-amino, 4-methoxy groups and a phenylethyl ring with methoxy groups at 2, 4 and 6-positions showed optimum biological activity. Biological evaluation of the activity of these compounds show that these compounds are highly active against a wide variety of human tumor cell lines including those that are resistant to many of the currently used chemotherapeutic agents.

Discovery of novel (2-(substituted benzylsulfonyl) ethyl) substituted benzenes as highly potent anti-cancer agents

251st National Meeting (2016)

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