880-14-8Relevant articles and documents
Synthesis of new thioureas derivatives and evaluation of their efficacy as proliferation inhibitors in mcf-7 breast cancer cells by using99m tc-mibi radiotracer
Hormati, Ahmad,Shiran, Jafar Abbasi,Molazadeh, Mikaeil,Kaboudin, Babak,Ahmadpour, Sajjad
, p. 766 - 778 (2021/04/02)
Background & Objective: Anti-tumor activity of some thioureas derivatives is well documented in literature and received considerable attention. The present study aims to synthesize and characterize some novel thioureas and carbonylthioureas as anti-tumor
Synthesis, molecular docking and biological evaluation of N,N-disubstituted 2-aminothiazolines as a new class of butyrylcholinesterase and carboxylesterase inhibitors
Makhaeva, Galina F.,Boltneva, Natalia P.,Lushchekina, Sofya V.,Serebryakova, Olga G.,Stupina, Tatyana S.,Terentiev, Alexey A.,Serkov, Igor V.,Proshin, Alexey N.,Bachurin, Sergey O.,Richardson, Rudy J.
, p. 1050 - 1062 (2016/02/19)
A series of 31 N,N-disubstituted 2-amino-5-halomethyl-2-thiazolines was designed, synthesized, and evaluated for inhibitory potential against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and carboxylesterase (CaE). The compounds did not inhibit AChE; the most active compounds inhibited BChE and CaE with IC50 values of 0.22-2.3 μM. Pyridine-containing compounds were more selective toward BChE; compounds with the para-OMe substituent in one of the two dibenzyl fragments were more selective toward CaE. Iodinated derivatives were more effective BChE inhibitors than brominated ones, while there was no influence of halogen type on CaE inhibition. Inhibition kinetics for the 9 most active compounds indicated non-competitive inhibition of CaE and varied mechanisms (competitive, non-competitive, or mixed-type) for inhibition of BChE. Docking simulations predicted key binding interactions of compounds with BChE and CaE and revealed that the best docked positions in BChE were at the bottom of the gorge in close proximity to the catalytic residues in the active site. In contrast, the best binding positions for CaE were clustered rather far from the active site at the top of the gorge. Thus, the docking results provided insight into differences in kinetic mechanisms and inhibitor activities of the tested compounds. A cytotoxicity test using the MTT assay showed that within solubility limits (30 μM), none of the tested compounds significantly affected viability of human fetal mesenchymal stem cells. The results indicate that a new series of N,N-disubstituted 2-aminothiazolines could serve as BChE and CaE inhibitors for potential medicinal applications.
Heterocyclization of N-hetaryl-N′-(prop-2-en-1-yl)thioureas by the action of sulfuryl chloride
Zborovskii,Orysyk,Staninets,Rusanov,Chernega
, p. 1030 - 1034 (2008/03/13)
Cyclization of N-hetaryl-N′-(prop-2-en-1-yl)thioureas by the action of sulfuryl chloride leads to the formation of the corresponding 2-hetarylimino-5-chloromethylthiazolidine hydrochlorides which are converted into the free bases by treatment with aqueous
