Cytochrome P450 enzymes are a superfamily of hemoproteins involved in the metabolism and detoxification of endogenous and exogenous compounds. Some P450s participate in bio-activation of certain procarcinogens that leads to the production of carcinogens. This has resulted in their popularity as targets in cancer research. Developing selective and potent mechanism-based inhibitors for these enzymes is expected to be the key to understanding their mechanisms of action as well as producing anticancer agents. Our group has shown that certain aryl and aryl-alkyl acetylenes act as inhibitors of these enzymes. In an attempt to increase the number of selective P450 inhibitors available for enzymatic studies, a novel group of dibenzofuranol ethers possessing an methyl and acetylene moiety, have been designed.

Design and syntheses of new dibenzofuranol ether derivatives as potential cytochrome P450 inhibitors

255th National Meeting (2018)

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