期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 69, 期 -, 页码 191-200出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.07.056
关键词
AKT; ABL; Protein kinase; HUVECs; Rat thoracic aorta rings
资金
- National Nature Science Foundation of China [21172134]
- National Scientific and Technological Major Project of Ministry of Science and Technology of China [2011ZX09401-015]
- Academic Award for Doctoral Postgraduate of Ministry of Education of China [20110131110037]
A novel series of 4-amino-2-(thio)phenol derivatives were well synthesized. The preliminary biological test revealed that several compounds displayed high specific protein kinase and angiogenesis inhibitory activities compared with previous work mainly because of the substitution of sulfonamide structure for amide fragment. Among which, compound 5i was identified to inhibit protein kinase B/AKT (IC50 = 1.26 mu M) and ABL tyrosine kinase (IC50 = 1.50 mu M) effectively. Meanwhile, compound 5i demonstrated competitive in vitro antiangiogenic activities to Pazopanib in both human umbilical vein endothelial cell (HUVEC) tube formation assay and the rat thoracic aorta rings test. (C) 2013 Elsevier Masson SAS. All rights reserved.
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