Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 124, Issue -, Pages 229-236Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.08.043
Keywords
Polo-like kinase 1; Polo-box domain; Small molecular inhibitor; Halogenosulfamoylphenyl acylthiourea; Binding affinity; In vitro assay
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Funding
- National Natural Science Foundation of China [21573012, 21633001, 91313302]
- Ministry of Science and Technology of China [2015CB910300]
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Thiourea derivatives have drawn much attention for their latent capacities of biological activities. In this study, we designed acylthiourea compounds as polo-like kinase 1 (Plk1) polo-box domain (PBD) inhibitors. A series of acylthiourea derivatives without pan assay interference structure (PAINS) were synthesized. Four compounds with halogen substituents exhibited binding affinities to Plk1 PBD in low micromole range. The most potent compound (3v) showed selectivity over other subtypes of Plk PBDs and inhibited the kinase activity of full-length Plk1. (C) 2016 Elsevier Masson SAS. All rights reserved.
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