93691-33-9

Upstream product

• 3811-20-9 1-(4-(iso-propyl)benzylidene)thiosemicarbazide 
• 555-16-8 4-nitrobenzaldehdye 
• 79-11-8 chloroacetic acid 
• 74268-25-0 4-nitro-benzaldehyde-(S-methyl-iso thiosemicarbazone) 
• 68-11-1 mercaptoacetic acid 
• 5470-48-4 para-nitrobenzaldehyde thiosemicarbazone 
• 105-39-5 chloroacetic acid ethyl ester 
• 180864-33-9 (2E)-2-[(4-nitrophenyl)methylidene]hydrazine-1-carbothioamide 
• 105-36-2 ethyl bromoacetate 

Relevant academic research and scientific papers

Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents

4-Thiazolidinone analogs 1-20 were synthesized, characterized by 1H NMR and EI-MS and investigated for urease inhibitory activity. All twenty (20) analogs exhibited varied degree of urease inhibitory potential with IC50 values 1.73-69.65 μM, if compared with standard thiourea having IC50 value of 21.25 ± 0.15 μM. Among the series, eight derivatives 3, 6, 8, 10, 15, 17, 19, and 20 showed outstanding urease inhibitory potential with IC50 values of 9.34 ± 0.02, 14.62 ± 0.03, 8.43 ± 0.01, 7.3 ± 0.04, 2.31 ± 0.002, 5.75 ± 0.003, 8.81 ± 0.005, and 1.73 ± 0.001 μM, respectively, which is better than the standard thiourea. The remaining analogs showed good to excellent urease inhibition. The binding interactions of these compounds were confirmed through molecular docking studies.

Design, synthesis and biological evaluation of thiazolidinone derivatives as potential EGFR and HER-2 kinase inhibitors

Two series of thiazolidinone derivatives designing for potential EGFR and HER-2 kinase inhibitors have been discovered. Some of them exhibited significant EGFR and HER-2 inhibitory activity. Compound 2-(2-(5-bromo-2-hydroxybenzylidene)hydrazinyl)thiazol-4(5H)-one (12) displayed the most potent inhibitory activity (IC50 = 0.09 μM for EGFR and IC50 = 0.42 μM for HER-2), comparable to the positive control erlotinib. Docking simulation was performed to position compound 12 into the EGFR active site to determine the probable binding model. Antiproliferative assay results indicating that some of the thiazolidinone derivatives own high antiproliferative activity against MCF-7. Compound 12 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent.