354811-97-5

Upstream product

• 586-37-8 1-(3-Methoxyphenyl)ethanone 
• 474843-37-3 3-chloro-3-(3-methoxyphenyl)prop-2-enenitrile 
• 2365-48-2 Methyl thioglycolate 
• 1055176-04-9 (Z)-3-Chloro-3-(3-methoxy-phenyl)-acrylonitrile 

Downstream Products

• 354812-19-4 3-amino-5-(3-methoxyphenyl)-2-thiophenecarboxylic acid 
• 1450979-98-2 3-(3-methoxybenzyl)-6-(3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one 
• 1450979-99-3 3-(3-hydroxybenzyl)-6-(3-hydroxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one 
• 1450979-90-4 methyl 3-{[(1E)-(dimethylamino)methylidene]amino}-5-(3-methoxyphenyl)thiophene-2-carboxylate 
• 874818-79-8 6-(3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one 
• 354811-98-6 3-amino-5-(3-methoxyphenyl)thiophene-2-carboxamide 

Relevant academic research and scientific papers

One-pot synthesis of 2-substituted thieno[3,2-b]indoles from 3-aminothiophene-2-carboxylates through in situ generated 3-aminothiophenes

A convenient protocol for one-pot synthesis of thieno[3,2-b]indoles, bearing aromatic, thien-2-yl or styryl fragments at C-2 position, from easily accessible 5-substituted 3-aminothiophene-2-carboxylates using the Fischer indolization reaction, was develo

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.

Synthesis and biological evaluation of thieno[3,2-d]- pyrimidinones, thieno[3,2-d]pyrimidines and quinazolinones: Conformationally restricted 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors

In this study, a series of conformationally restricted thieno[3,2-d] pyrimidinones, thieno[3,2-d]pyrimidines and quinazolinones was designed and synthesized with the goal of improving the biological activity as 17β-hydroxysteroid dehydrogenase type 2 inhi

Discovery and SAR of a novel selective and orally bioavailable nonpeptide classical competitive inhibitor class of protein-tyrosine phosphatase 1B

Reversible phosphorylation and dephosphorylation of key proteins on tyrosine residues are important parts of intracellular signaling triggered by hormones and other agents. Recent knock-out studies in mice have identified PTP1B as a potential target for t

Novel Compounds

The invention relates to heteroaromatic carboxamides of formula (I), wherein A, R1, R2 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.