Design, synthesis, and evaluation of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives as Aurora kinase inhibitors
- 주제(키워드) 1 , 2 , 3-Triazole , Anticancer , Aurora kinase , Click chemistry , Hinge-binder
- 등재 SCIE, SCOPUS
- 발행기관 Elsevier Ltd
- 발행년도 2016
- 총서유형 Journal
- URI http://www.dcollection.net/handler/ewha/000000126605
- 본문언어 영어
- Published As http://dx.doi.org/10.1016/j.bmc.2016.03.042
- 저작권 이화여자대학교 논문은 저작권에 의해 보호받습니다.
초록/요약
A series of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives were designed, synthesized, and evaluated for the Aurora kinase inhibitory activities. The novel hinge-binder tethered 1,2,3-triazolylsalicylamide scaffold was effectively assembled by Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC). A variety of alkynes with hinge binders were used to search proper structures-binding relationship to the hinge region. The synthesized 1,2,3-triazolylsalicylamide derivatives showed significant Aurora kinase inhibitory activity. In particular, 8a inhibited Aurora A kinase with an IC50 value of 0.284μM, whereas 8m inhibited Aurora B kinase with an IC50 value of 0.364μM. © 2016 Elsevier Ltd.
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