کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1379091 | 982017 | 2006 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of trans-3,4′-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A novel series of Akt/PKB inhibitors derived from a screening lead (1) has been prepared. The novel trans-3,4′-bispyridinylethylenes described herein are potent inhibitors of Akt/PKB with IC50 values in the low double-digit nanomolar range against Akt1. Compound 2q shows excellent selectivity against distinct families of kinases such as tyrosine kinases and CAMK, and displays poor to modest selectivity against closely related kinases in the AGC and CMGC families. The cellular activities including inhibition of cell growth and phosphorylation of downstream target GSK3 are also described. The X-ray structure of compound 2q complexed with PKA in the ATP binding site was determined.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 6, 15 March 2006, Pages 1679–1685
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 6, 15 March 2006, Pages 1679–1685
نویسندگان
Qun Li, Tongmei Li, Gui-Dong Zhu, Jianchun Gong, Akiyo Claibone, Chris Dalton, Yan Luo, Eric F. Johnson, Yan Shi, Xuesong Liu, Vered Klinghofer, Joy L. Bauch, Kennan C. Marsh, Jennifer J. Bouska, Shannon Arries, Ron De Jong, Tilman Oltersdorf,