Goyal Navneet, Bongay-Williams Kyla, Do Camilla, Perry Timothy, Kantrow Eleanor, Hill-Odom Miriam, Sridhar Jayalakshmi, Foroozesh Maryam
Department of Chemistry, Xavier University of Louisiana, New Orleans, Louisiana 70125.
J Undergrad Chem Res. 2018 Fall;17(4):102-104.
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.
细胞色素P450酶是一族血红蛋白，参与内源性和外源性化合物的代谢及解毒过程。P450酶参与某些前致癌物的生物活化，导致致癌物质的产生。这使得P450酶成为癌症研究中的热门靶点。开发针对这些酶的选择性和强效的基于机制的抑制剂，有望成为理解其作用机制以及开发潜在抗癌药物的关键。我们的研究小组已经表明，某些芳基和芳基烷基乙炔可作为这些酶的抑制剂。为了增加可用于酶学研究的选择性P450抑制剂的数量，我们成功设计并合成了五种新型二苯并呋喃醚和酯。
