6-Amino-2,4,5-trimethylpyridin-3-ols: A new general synthetic route and antiangiogenic activity
- Authors
- Kim, Dong-Guk; Kang, Youra; Lee, Hyunji; Lee, Eun Kyung; Tae-gyu Nam; Kim, Jung-Ae; Jeong, Byeong-Seon
- Issue Date
- May-2014
- Publisher
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
- Keywords
- Aminopyridinol; Angiogenesis; Antiangiogenic; Antitumor; Chick chorioallantoic membrane assay
- Citation
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.78, pp.126 - 139
- Indexed
- SCIE
SCOPUS
- Journal Title
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Volume
- 78
- Start Page
- 126
- End Page
- 139
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/22878
- DOI
- 10.1016/j.ejmech.2014.03.045
- ISSN
- 0223-5234
- 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.
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