کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1394168 1501138 2014 14 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
6-Amino-2,4,5-trimethylpyridin-3-ols: A new general synthetic route and antiangiogenic activity
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
6-Amino-2,4,5-trimethylpyridin-3-ols: A new general synthetic route and antiangiogenic activity
چکیده انگلیسی


• A general synthetic strategy for 6-amino-2,4,5-trimethylpyridin-3-ols was developed.
• A wider range of aminopyridinols can be prepared by the new synthetic strategy.
• Some aminopyridinols show high level of antiangiogenic activities in CAM assay.

A new synthetic strategy for preparation of a wide range of 6-amino-2,4,5-trimethylpyridin-3-ols from pyridoxine·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.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 78, 6 May 2014, Pages 126–139
نویسندگان
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