61291-89-2

Upstream product

• 26197-93-3 p-bromothiobanzamide 
• 609-15-4 ethyl 2-chloro-3-oxo-butyrate 
• 623-00-7 4-bromobenzenecarbonitrile 

Downstream Products

• 83432-73-9 1-(2-(4-bromophenyl)-4-methylthiazol-5-carbonyl)-4-phenylthiosemicarbazide 
• 1428354-67-9 1-(2-(4-bromophenyl)-4-methylthiazol-5-carbonyl)-4-methylthiosemicarbazide 
• 1428354-70-4 4-allyl-1-(2-(4-bromophenyl)-4-methylthiazol-5-carbonyl)-thiosemicarbazide 
• 83432-82-0 3-(2-(4-bromophenyl)-4-methylthiazol-5-yl)-4-phenyl-1H-1,2,4-triazol-5(4H)-thione 
• 1428354-73-7 3-(2-(4-bromophenyl)-4-methylthiazol-5-yl)-4-methyl-1H-1,2,4-triazol-5(4H)-thione 
• 1428354-75-9 4-allyl-3-(2-(4-bromophenyl)-4-methylthiazol-5-yl)-1H-1,2,4-triazol-5(4H)-thione 
• 1428354-60-2 5-(2-(4-bromophenyl)-4-methylthiazol-5-yl)-1,3,4-oxadiazol-2(3H)-thione 
• 61291-93-8 [2-(4-bromo-phenyl)-4-methyl-thiazol-5-yl]-methanol 

Relevant academic research and scientific papers

Design, synthesis, biological evaluation, common feature pharmacophore model and molecular dynamics simulation studies of ethyl 4-(phenoxymethyl)-2-phenylthiazole-5-carboxylate as Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) inhi

SHP2 is a non-receptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene involved in cell death pathway (PD-1/PD-L1) and cell growth and differentiation pathway (MAPK). Moreover, mutations in SHP2 have been implicated in Leopard syndrome (LS),

Design, synthesis and biological evaluation of novel thiazole-derivatives as mitochondrial targeting inhibitors of cancer cells

Mitochondria are pivotal energy production sources for cells to maintain necessary metabolism activities. Targeting dysfunctional mitochondrial features has been a hotspot for mitochondrial-related disease researches. Investigation with cancerous mitochondrial metabolism is a continuing concern within tumor therapy. Herein, we set out to assess the anti-cancer activities of a novel family of TPP-thiazole derivatives based on our earlier research on mitochondrial targeting agents. Specifically, we designed and synthesized a series of TPP-thiazole derivatives and revealed by the MTT assay that most synthesized compounds effectively inhibited three cancer cell lines (HeLa, PC3 and MCF-7). After structure modifications, we explored the SAR relationships and identified the most promising compound R13 (IC50 of 5.52 μM) for further investigation. In the meantime, we performed ATP production assay to assess the selected compounds inhibitory effect on HeLa cells energy production. The results displayed the test compounds significantly restrained ATP production of cancer cells. Overall, we have designed and synthesized a series of compounds which exhibited significant cytotoxicity against cancer cells and effectively inhibited mitochondrial energy production.

Identification of protein tyrosine phosphatase 1B (PTP1B) inhibitors through De Novo Evoluton, synthesis, biological evaluation and molecular dynamics simulation

Protein tyrosine phosphatase 1B (PTP1B) is a widely expressed 50 kDa enzyme and the first intracellular PTP to be purified from human placental tissue. It has been proved that protein tyrosine phosphatase 1B played a significant role in the negative regul

miRNA biosynthesis inhibitor

The invention provides a compound shown as a formula I, or a conformational isomer thereof, or an optical isomer thereof, or a pharmaceutically acceptable salt thereof. The compound can be tightly combined with related binding proteins in an miRNA biosynthesis process and can effectively inhibit the synthesis of miRNA-21. The prepared active compound provided by the invention can be used as an miRNA-21 inhibitor, and further as a potential drug for treating malignant tumors. The formula I is shown in the description.

2-substitution-4-methyl-5-(4, 5-thiazoline-2-base)-1, 3-thiazole compound, method for preparing same and evaluation of biological activity

The invention belongs to the field of technologies for chemically synthesizing thiazole derivatives and evaluating the biological activity, and relates to a 2-substitution-4-methyl-5-(4, 5-thiazoline-2-base)-1, 3-thiazole compound shown as a formula I, and further provides a method for preparing 2-substitution-4-methyl-5-(4, 5-thiazoline-2-base)-1, 3-thiazole and evaluation of the biological activity for inhibiting the activity of urease and inhibiting the activity of Escherichia coli, Bacillus subtilis and Staphylococcus aureas. The 2-substitution-4-methyl-5-(4, 5-thiazoline-2-base)-1, 3-thiazole compound, the method and the evaluation have the advantages that the 2-substitution-4-methyl-5-(4, 5-thiazoline-2-base)-1, 3-thiazole compound has certain biological activity, and accordingly the 2-substitution-4-methyl-5-(4, 5-thiazoline-2-base)-1, 3-thiazole compound, the method and the evaluation have excellent application prospects in the industries of medicines, pesticides and the like.

Design and optimization of hybrid of 2,4-diaminopyrimidine and arylthiazole scaffold as anticancer cell proliferation and migration agents

Therapeutics of metastatic or triple-negative breast cancer are still challenging in clinical. Herein we demonstrated the design and optimization of a series of hybrid of 2,4-diaminopyrimidine and arylthiazole derivatives for their anti-proliferative properties against two breast cancer cell lines (MCF-7 as human breast cancer and MDA-MB-231 as triple-negative breast cancer). More importantly, some of those compounds with potent antiproliferative activities also indicated excellent inhibitory activities against MDA-MB-231 cell migration. These results suggested that the new series of hybridation of aryl-thiazoles and aminopyrimidines could be identified and developed as novel highly potential anticancer agents against the triple-negative breast cancer as well as metastatic one in the future.

HETEROCYCLIC COMPOUNDS AS MODULATORS OF PEROXISOME PROLIFERATOR ACTIVATED RECEPTORS, USEFUL FOR THE TREATMENT AND/OR PREVENTION OF DISORDERS MODULATED BY A PPAR

The present invention is directed to a compound of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.