Citation

Goyal N, Bongay-Williams K, Do C, Perry T, Kantrow E, Hill-Odom M, Sridhar J, Foroozesh M. Journal of Undergraduate Chemistry Research 2018; 17(4): 102-104.

Copyright

(Copyright © 2018)

DOI

unavailable

PMID

31363349

PMCID

PMC6667160

Abstract

Cytochrome P450 enzymes are a superfamily of hemoproteins involved in the metabolism and detoxification of endogenous and exogenous compounds. P450s are involved in the bioactivation of certain procarcinogens leading to the production of carcinogenic species. This has resulted in P450s' 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, developing potential 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, five novel dibenzofuran ethers and esters have been designed and synthesized successfully.

Language: en

Keywords

Enzyme Inhibitors; Metabolism; Acetylenes; Cytochrome P450 Enzymes; Organic Synthesis; Propargyl Pyridinyl Ethers; Suicide Inhibitors