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Bioorg Med Chem. 2014 Sep 1;22(17):4855-66. doi: 10.1016/j.bmc.2014.06.047. Epub 2014 Jun 30.

Click approach to the discovery of 1,2,3-triazolylsalicylamides as potent Aurora kinase inhibitors.

Author information

1
College of Pharmacy & Graduate School of Pharmaceutical Sciences, Global Top 5 Research Program, Ewha Womans University, 11-1 Daehyun-Dong, Seodaemun-Gu, Seoul 120-750, Republic of Korea.
2
Department of Pharmacy, College of Pharmacy, Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan, Kyeonggi-do 426-791, Republic of Korea.
3
College of Pharmacy & Graduate School of Pharmaceutical Sciences, Global Top 5 Research Program, Ewha Womans University, 11-1 Daehyun-Dong, Seodaemun-Gu, Seoul 120-750, Republic of Korea. Electronic address: ryuj@ewha.ac.kr.

Abstract

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 0.37μM. The critical role of phenolic -OH in the binding was confirmed by a molecular modeling study.

KEYWORDS:

1,2,3-Triazole; Anticancer; Aurora kinase; Click chemistry; Library

PMID:
25042560
DOI:
10.1016/j.bmc.2014.06.047
[Indexed for MEDLINE]

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