View : 16 Download: 0

trans-Stilbenoids: Potent and selective inhibitors for human cytochrome P450 1B1

Title
trans-Stilbenoids: Potent and selective inhibitors for human cytochrome P450 1B1
Authors
Chun Y.-J.Lim C.Ohk S.O.Lee J.M.Lee J.H.Choi S.Kim S.
Ewha Authors
최선
SCOPUS Author ID
최선scopus
Issue Date
2011
Journal Title
MedChemComm
ISSN
2040-2503JCR Link
Citation
vol. 2, no. 5, pp. 402 - 405
Indexed
SCIE; SCOPUS WOS scopus
Abstract
On the basis of our previous insights into the structural requirements of stilbenoids for the inhibition of cytochrome P450 1B1 (CYP1B1), a series of 2,4-dimethoxy group-containing stilbenes was prepared and evaluated for their inhibitory effects on the activity of CYP1s with the ultimate goal of identifying a potent and selective CYP1B1 inhibitor. Among the thirteen derivatives prepared, five compounds exhibited similar or greater potency compared to the previous lead compound, 2,4,3′,5′- tetramethoxystilbene (2,4,3′,5′-TMS), in inhibiting CYP1B1. In particular, 2,2′,3′,4,6′-pentamethoxystilbene was found to be a more selective and more potent CYP1B1 inhibitor than 2,4,3′,5′- TMS. 2,4,2′,6′-TMS showed remarkably potent inhibitory activity against CYP1B1 (IC 50 = 1.77 ± 0.14 nM) and also had a very high selectivity toward CYP1 isoenzymes. Molecular modeling was performed to determine the key molecular interactions with the CYP1B1 and CYP1A2 structures. On the basis of these structural and biological studies, the design of more potent and more selective drug-like derivatives can be envisaged. © The Royal Society of Chemistry 2011.
DOI
10.1039/c0md00242a
Appears in Collections:
약학대학 > 약학과 > Journal papers
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE