2131-62-6Relevant articles and documents
Synthesis and photophysical characterization of proton transfer-based thiourea derivatives: Potential application as colorimetric naked-eye chemosensor for fluoride detection in solution
Da Silva, Cláudia B.,Kroetz, Thais,Santos, Fabiano S.,Rodembusch, Fabiano S.
, p. 1830 - 1841 (2017)
Two new thiourea derivatives were synthesized through the reaction of photoactive aminohydroxybenzazoles and p-isothiocyanate benzoic acid via nucleophilic addition reaction. The compounds were characterized using high resolution mass spectrometry with el
2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site
Bestgen, Beno?t,Krimm, Isabelle,Kufareva, Irina,Kamal, Ahmed Ashraf Moustafa,Seetoh, Wei-Guang,Abell, Chris,Hartmann, Rolf W.,Abagyan, Ruben,Cochet, Claude,Le Borgne, Marc,Engel, Matthias,Lomberget, Thierry
, p. 1803 - 1816 (2019/03/07)
CK2 is a ubiquitous Ser/Thr protein kinase involved in the control of various signaling pathways and is known to be constitutively active. In the present study, we identified aryl 2-aminothiazoles as a novel class of CK2 inhibitors, which displayed a non-ATP-competitive mode of action and stabilized an inactive conformation of CK2 in solution. Enzyme kinetics studies, STD NMR, circular dichroism spectroscopy, and native mass spectrometry experiments demonstrated that the compounds bind in an allosteric pocket outside the ATP-binding site. Our data, combined with molecular docking studies, strongly suggested that this new binding site was located at the interface between the αC helix and the flexible glycine-rich loop. A first hit optimization led to compound 7, exhibiting an IC50 of 3.4 μM against purified CK2α in combination with a favorable selectivity profile. Thus, we identified a novel class of CK2 inhibitors targeting an allosteric pocket, offering great potential for further optimization into anticancer drugs.
Synthesis and biological evaluation of arylthiourea derivatives with antitubercular activity
Luo, Rusong,Laitinen, Tuomo,Teng, Liyan,Nevalainen, Tapio,Lahtela-Kakkonen, Maija,Zheng, Baofu,Wang, Honghai,Poso, Antti,Zhang, Xuelian
, p. 640 - 650 (2013/08/23)
Tuberculosis (TB) is a contagious disease caused by Mycobacterium tuberculosis (M. tuberculosis), and remains one of the most life-threatening plagues for public health in the world. The emergence of drug resistant strains of TB and co-infection with HIV has further complicated TB treatment. Here, the synthesis and characterizaton of a series of compounds were described, and these were followed by evaluating for their antibacterial activity against M. tuberculosis. Several novel arylthiourea derivatives exhibited excellent activity (lowest MIC=0.09 μg/ml) against M. tuberculosis including drug resistant strains of M. tuberculosis. The results suggest that these compounds are promising candidates for new anti-TB agent development.
