期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 3, 页码 518-523出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.12.030
关键词
Nimesulide; 1,2,3-Triazole; Azide; Alkyne; Anticancer activity
A new hybrid template has been designed by integrating the structural features of nimesulide and the 1,2,3-triazole moiety in a single molecular entity at the same time eliminating the problematic nitro group of nimesulide. The template has been used for the generation of a library of molecules as potential anticancer agents. A mild and greener CuAAC approach has been used to synthesize these compounds via the reaction of 4-azido derivative of nimesulide and terminal alkynes in water. Three of these compounds showed promising growth inhibition (IC50 similar to 6-10 mu M) of A549, HepG2, HeLa and DU145 cancer cell lines but no significant effects on HEK293 cell line. They also inhibited PDE4B in vitro (60-70% at 10 mu M) that was supported by the docking studies (PLP score 87-94) in silico. (C) 2016 Elsevier Ltd. All rights reserved.
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