57466-68-9

Upstream product

• 39812-29-8 <3-chloro-3-(4-methoxyphenyl)-2-propen-1-yliden> dimethyliminium perchlorate 
• 100-06-1 1-(4-methoxyphenyl)ethanone 
• 14063-79-7 3-chloro-3-(4-methoxyphenyl)acrylaldehyde 
• 93-61-8 N-methyl-N-phenylformamide 
• 68-12-2 N,N-dimethyl-formamide 
• 72806-45-2 1-p-Anisyl-1-chlor-propen-3-al-oxim 

Downstream Products

• 37572-23-9 3-amino-5-(4-methoxyphenyl)thiophene-2-carboxylic acid methyl ester 
• 1253594-43-2 5-(4-methoxyphenyl)-3-thiopheneamine 
• 6525-97-9 3-amino-5-(4-methoxyphenyl)isoxazole 
• 3672-47-7 3-oxo-3-(4'-methoxyphenyl)propanenitrile 
• 1610730-66-9 2-(4-chlorophenyl)-5-{[6-(4-methoxyphenyl)thieno[3,2-d]pyrimidin-4-yl]thio}-1,3,4-oxadiazole 
• 1610730-65-8 2-{[6-(4-methoxyphenyl)thieno[3,2-d]pyrimidin-4-yl]thio}-5-phenyl-1,3,4-oxadiazole 
• 1610730-78-3 4-chloro-6-(4-methoxyphenyl)thieno[3,2-d]pyrimidin-2-amine 

Relevant academic research and scientific papers

Novel benzenesulfonamide-bearing pyrazoles and 1,2,4-thiadiazoles as selective carbonic anhydrase inhibitors

Two series comprising 20 novel benzenesulfonamides bearing thioureido-linked pyrazole 8 and amino-1,2,4-thiadiazole 10 were synthesized and assayed as human carbonic anhydrase (hCA) inhibitors against isoforms I and II as well as the tumor-associated isof

Deadly KCN and pricey metal free track for accessing β-ketonitriles employing mild reaction conditions

A one pot synthesis of β-ketonitriles from readily accessible 3-chloropropenals using economically benign iodine, aqueous ammonia and sodium hydroxide solution, employing mild reaction conditions have been described. This report presents a convenient, inexpensive, highly toxic-matter-free and eco-friendly approach for β-ketonitriles.

Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors

The clinical evidence for the success of tyrosine kinase inhibitors in combination with microtubule-targeting agents prompted us to design and develop single agents that possess both epidermal growth factor receptor (EGFR) kinase and tubulin polymerization inhibitory properties. A series of 6-aryl/heteroaryl-4-(3′,4′,5′-trimethoxyanilino)thieno[3,2-d]pyrimidine derivatives were discovered as novel dual tubulin polymerization and EGFR kinase inhibitors. The 4-(3′,4′,5′-trimethoxyanilino)-6-(p-tolyl)thieno[3,2-d]pyrimidine derivative 6g was the most potent compound of the series as an antiproliferative agent, with half-maximal inhibitory concentration (IC50) values in the single- or double-digit nanomolar range. Compound 6g bound to tubulin in the colchicine site and inhibited tubulin assembly with an IC50 value of 0.71 μM, and 6g inhibited EGFR activity with an IC50 value of 30 nM. Our data suggested that the excellent in vitro and in vivo profile of 6g may be derived from its dual inhibition of tubulin polymerization and EGFR kinase.

Exploring the chemical space of ureidothiophene-2-carboxylic acids as inhibitors of the quorum sensing enzyme PqsD from Pseudomonas aeruginosa

Pseudomonas aeruginosa employs a quorum sensing (QS) communication system that makes use of small diffusible molecules. Among other effects, the QS system coordinates the formation of biofilm which decisively contributes to difficulties in the therapy of

THIOETHER DERIVATIVES AS PROTEIN KINASE INHIBITORS

The present invention relates to thioether derivatives (1) as protein kinase inhibitors, which are useful for the treatment, relieve and/or prevention of diseases associated with abnormal and hyperproliferation of cells in a mammal, especially humans, and which are particularly useful for the treatment of all forms of cancer.

Novel small molecule inhibitors targeting the "switch region" of bacterial RNAP: Structure-based optimization of a virtual screening hit

Rising resistance against current antibiotics necessitates the development of antibacterial agents with alternative targets. The "switch region" of RNA polymerase (RNAP), addressed by the myxopyronins, could be such a novel target site. Based on a hit can

Combining in silico and biophysical methods for the development of pseudomonas aeruginosa quorum sensing inhibitors: An alternative approach for structure-based drug design

The present work deals with the optimization of an inhibitor of PqsD, an enzyme essential for Pseudomonas aeruginosa quorum sensing apparatus. Molecular docking studies, supported by biophysical methods (surface plasmon resonance, isothermal titration cal

Synthesis of a novel series of thieno[3,2-d]pyrimidin-4-(3H)-ones

2-Aminothieno[3,2-d]pyrimidin-4-ones were synthesized in one step by condensation of 3-amino(benzo)thiophene car-boxylate with chloroformamidine hydrochloride. Georg Thieme Verlag Stuttgart.

Synthesis of selenophene analogues of the tacrine series: Comparison of classical route and microwave irradiation

New 3-amino-2-selenophenecarbonitriles condensed with cyclanones to afford, in one step, analogues of Tacrine. A comparison between classical heating and microwave irradiation for the Friedlaender condensation is presented. Georg Thieme Verlag Stuttgart.

The discovery and optimization of pyrimidinone-containing MCH R1 antagonists

Optimization of a series of constrained melanin-concentrating hormone receptor 1 (MCH R1) antagonists has provided compounds with potent and selective MCH R1 activity. Details of the optimization process are provided and the use of one of the compounds in