Click approach to the discovery of 1,2,3-triazolylsalicylamides as potent Aurora kinase inhibitors
- 주제(키워드) Aurora kinase , Click chemistry , Library , 1 , 2 , 3-Triazole , Anticancer
- 등재 SCIE, SCOPUS
- 발행기관 PERGAMON-ELSEVIER SCIENCE LTD
- 발행년도 2014
- 총서유형 Journal
- URI http://www.dcollection.net/handler/ewha/000000108791
- 본문언어 영어
- Published As http://dx.doi.org/10.1016/j.bmc.2014.06.047
초록/요약
A series of 1,2,3-triazolylsalicylamide derivatives has been developed from the antiproliferative agent 7 and was evaluated for their Aurora kinase inhibitory activity. The novel 1,2,3-triazolylsalicylamide scaffold could be readily assembled by Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition, allowing rapid access to the structurally diverse analogues. The synthesized 1,2,3-triazolylsalicylamide derivatives revealed a significant Aurora kinase inhibitory activity. In particular, 8g inhibited Aurora A with IC50 values of 0.37 mu M. The critical role of phenolic -OH in the binding was confirmed by a molecular modeling study. (C) 2014 Elsevier Ltd. All rights reserved.
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