6-Amino-2,4,5-trimethylpyridin-3-ols: A new general synthetic route and antiangiogenic activity

Title
6-Amino-2,4,5-trimethylpyridin-3-ols: A new general synthetic route and antiangiogenic activity
Author(s)
정병선김동국강유라이현지이은경남태규[남태규]김정애
Keywords
PALLADIUM-CATALYZED AMINATION; TYROSINE KINASE INHIBITORS; ENDOTHELIAL GROWTH-FACTOR; CELL-PROLIFERATION; BOND FORMATION; ARYL HALIDES; IN-VITRO; ANGIOGENESIS; MECHANISM; PROPOLIS
Issue Date
201405
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citation
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.78, pp.126 - 139
Abstract
A new synthetic strategy for preparation of a wide range of 6-amino-2,4,5-trimethylpyridin-3-ols from pyridoxine center dot HCl via a six-step sequence has been developed. This approach features an introduction of various amino groups to C(6)-position of 3-benzyloxy-6-bromo-2,4,5-trimethylpyridine (13), a key intermediate, by a Buchwald-Hartwig amination reaction using palladium(0) transition metal, which certainly renders an expanded scope of amino substituents. Some analogs prepared using the methods described here showed high level of antiangiogenic and antitumor activities in chick chorioallantoic membrane (CAM) assay, demonstrating the potential of these new aminopyridinols as antiangiogenic agents. (C) 2014 Elsevier Masson SAS. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/32335http://dx.doi.org/10.1016/j.ejmech.2014.03.045
ISSN
0223-5234
Appears in Collections:
약학대학 > 약학부 > Articles
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