Design, synthesis, and discovery of novel trans-stilbene analogues as potent and selective human cytochrome P4501B1 inhibitors
- Authors
- Kim, S; Ko, H; Park, JE; Jung, S; Lee, SK; Chun, YJ
- Issue Date
- Jan-2002
- Publisher
- AMER CHEMICAL SOC
- Citation
- JOURNAL OF MEDICINAL CHEMISTRY, v.45, no.1, pp 160 - 164
- Pages
- 5
- Journal Title
- JOURNAL OF MEDICINAL CHEMISTRY
- Volume
- 45
- Number
- 1
- Start Page
- 160
- End Page
- 164
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/25151
- DOI
- 10.1021/jm010298j
- ISSN
- 0022-2623
- Abstract
- A series of trans-stilbene derivatives containing a 3,5-dimethoxyphenyl moiety were prepared through a new efficient solution phase synthetic pathway, and their inhibitory activities were evaluated on human cytochrome P450s (CYP) 1A1, 1A2, and 1B1 to find a potent and selective CYP1B1 inhibitor. We found that a substituent at the 2-position of the stilbene skeleton plays a very important role in discriminating between CYP1As and CYP1B1. Among the compounds tested, the most selective and potent CYP1B1 inhibitor was 2,3',4,5'-tetramethoxystilbene, Compound 7j, 2-[2-(3,5-dimethoxy-phenyl)vinyl]thiophene, showed greater inhibitory activities but had a lower selectivity toward all of the CYP1s tested.
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