Synthesis and antiangiogenic activity of 6-amido-2,4,5-trimethylpyridin-3-ols

Title
Synthesis and antiangiogenic activity of 6-amido-2,4,5-trimethylpyridin-3-ols
Author(s)
정병선이현지수리드반스코타김동국빈재휘진유진[진유진]자야가우탐장현진남태규[남태규]김정애
Keywords
CHAIN-BREAKING ANTIOXIDANTS; TYROSINE KINASE INHIBITORS; ENDOTHELIAL GROWTH-FACTOR; TUMOR ANGIOGENESIS; AMINOPYRIDINOL ANTIOXIDANTS; ALPHA-TOCOPHEROL; THALIDOMIDE; 6-AMINO-3-PYRIDINOLS; 5-PYRIMIDINOLS; MECHANISMS
Issue Date
201407
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.24, no.14, pp.3131 - 3136
Abstract
We recently reported that 6-aminoalkyl-2,4,5-trimethylpyridin-3-ols, novel series of 6-aminopyridin-3-ol-based antioxidants, have high antiangiogenic activities. In pursuit of wider variety in the analogues, we here report the synthesis and antiangiogenic activities of 6-amidoalkyl-2,4,5-trimethylpyridin-3-ols, which would not be considered excellent antioxidants because of the poorer electron-donating effect of the C(6)-amido group than the corresponding C(6)-amino group. The selected 6-amido compounds showed up to several fold-higher antiangiogenic activities and up to an order of magnitude better antitumor activities in the chick embryo chorioallantoic membrane (CAM) assay than SU4312, a positive control. We also found that paracetamol, as a direct phenolic analogue of our simplest 6-amidopyridin-3-ol, showed a moderate level of antiangiogenic activity. We propose this study will offer a basis for a scaffold of novel angiogenesis inhibitors that can perturb angiogenesis-related pathologies. (C) 2014 Elsevier Ltd. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/31609http://dx.doi.org/10.1016/j.bmcl.2014.05.005
ISSN
0960-894X
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약학대학 > 약학부 > Articles
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