17537-76-7

Upstream product

• 123-11-5 4-methoxy-benzaldehyde 
• 100-06-1 1-(4-methoxyphenyl)ethanone 
• 15854-11-2 ethyl 2-amino-4-(4'-methoxyphenyl) thiophene-3-carboxylate 
• 77287-34-4 formamide 
• 16712-16-6 ammonium formate 
• 13455-80-6 2-cyano-3-(4-methoxy-phenyl)-crotonic acid ethyl ester 

Downstream Products

• 312584-53-5 4-chloro-5-(4-methoxyphenyl)thieno[2,3-d]pyrimidine 
• 1639810-22-2 C₁₆H₁₄N₂O₄S 
• 1018281-39-4 4-piperazin-1-yl-5-(4-methoxy-phenyl)-thieno[2,3-d]pyrimidine 
• 929417-75-4 N-(4-(5-(4-methoxy-phenyl)-7H-thieno[2,3-d]pyrimidin-4-ylamino)-benzenesulfonyl)-acetamide 

Relevant academic research and scientific papers

Identification of 4-methoxythieno[2,3-d]pyrimidines as FGFR1 inhibitors

Aim. To identify novel FGFR1 inhibitors using virtual screening approach. Methods. We used methods of organic synthesis, molecular docking via the Autodock 4.2.6 program package and in vitro biochemical tests with γ-32P. Results. In vitro experiments showed that 9 of 23 tested compounds possess inhibitory activity against FGFR1 with IC50 values in the range from 0.9 to 5.6 μM. Conclusions. Nine FGFR1 inhibitors were developed. The mode of compounds binding with the ATP-acceptor site was determined using molecular docking methods and the dependence of the compounds’ activity on the substituents R1, R4 and R5 was evaluated.

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.

Novel 4-oxothienopyrimidinyl propanoic acid derivatives as AMPactivated protein kinase (AMPK) activators

Adenosine 5′-monophosphate (AMP) activated protein kinase (AMPK) is a highly conserved sensor of cellular energy. AMPK has been recognized as a key regulator of mammalian metabolic function and has emerged as an attractive target for the treatment of meta

AXL KINASE INHIBITORS

Axl kinase inhibitory compounds are disclosed, as well as compositions and methods of using the same in the treatment of cancer and other conditions mediated by and/or associated with Axl kinase.

THIENOPYRIMIDINE DERIVATIVES AS POTASSIUM CHANNEL INHIBITORS

The present invention provides thienopyrimidine compounds which are potasium channels inhibitors. Pharmaceutical compositions comprising the compounds and their use in the treatment of arrhythmia are also provided.