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.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Song D,Park Y,Yoon J,Aman W,Hah JM,Ryu JSdoi
10.1016/j.bmc.2014.06.047subject
Has Abstractpub_date
2014-09-01 00:00:00pages
4855-66issue
17eissn
0968-0896issn
1464-3391pii
S0968-0896(14)00493-3journal_volume
22pub_type
杂志文章abstract：:Luteolin, 5,7-dihydroxy-2-(3,4-dihydroxyphenyl)-4H-chromen-4-one, has been proposed and proved to be a novel dopamine transporter (DAT) activator. In order to develop this potential of luteolin, a series of novel luteolin derivatives were designed, synthesized, and evaluated for their DAT agonistic activities, utilizi...
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