667909-71-9Relevant academic research and scientific papers
Identification of acylthiourea derivatives as potent Plk1 PBD inhibitors
Yun, Taikangxiang,Qin, Tan,Liu, Ying,Lai, Luhua
, p. 229 - 236 (2016/09/09)
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.
Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists
Xi, Ning,Bo, Yunxin,Doherty, Elizabeth M.,Fotsch, Christopher,Gavva, Narender R.,Han, Nianhe,Hungate, Randall W.,Klionsky, Lana,Liu, Qingyian,Tamir, Rami,Xu, Shimin,Treanor, James J.S.,Norman, Mark H.
, p. 5211 - 5217 (2007/10/03)
A thiazole derivative, 2-(2,6-dichlorobenzyl)-N-(4-isopropylphenyl) thiazole-4-carboxamide (1), was identified as a TRPV1 antagonist. We synthesized various thiazole analogs and evaluated them for their ability to block capsaicin- or acid-induced calcium influx in TRPV1-expressing CHO cells. The IC50 values of the most potent antagonists were ca. 0.050 μM in these assays.
