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Eur J Med Chem. 2013 Nov;69:191-200. doi: 10.1016/j.ejmech.2013.07.056. Epub 2013 Aug 29.

Discovery of 4-amino-2-(thio)phenol derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: synthesis and biological evaluation. Part II.

Author information

1
Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong 250012, PR China.

Abstract

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 μM) and ABL tyrosine kinase (IC₅₀ = 1.50 μM) 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.

KEYWORDS:

ABL; AKT; FHRYIUWAZBCUGX-UHFFFAOYSA-N; HUVECs; Protein kinase; Rat thoracic aorta rings

PMID:
24036042
DOI:
10.1016/j.ejmech.2013.07.056
[Indexed for MEDLINE]
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