519016-84-3

Upstream product

• 403-42-9 1-(4-fluorophenyl)ethanone 
• 109-77-3 malononitrile 
• 579-48-6 2-(1-(4-fluorophenyl)ethylidene)malononitrile 
• 456-04-2 2-Chloro-4'-fluoroacetophenone 
• 748818-01-1 2-[2-chloro-1-(4-fluoro-phenyl)-ethylidene]-malononitrile 

Downstream Products

• 384351-45-5 4-chloro-5-(4-fluorophenyl)thieno[2,3-d]pyrimidine 
• 1321618-77-2 3-fluoro-4-(5-(4-fluorophenyl)thieno[2,3-d]pyrimidin-4-yloxy)aniline 
• 1321618-87-4 N-(3-fluoro-4-(5-(4-fluorophenyl)thieno[2,3-d]pyrimidin-4-yloxy)phenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide 
• 35978-37-1 5-(4-fluorophenyl)thieno[2,3-d]pyrimidin-4(3H)-one 

Relevant academic research and scientific papers

Synthesis, in vivo anti-inflammatory, COX-1/COX-2 and 5-LOX inhibitory activities of new 2,3,4-trisubstituted thiophene derivatives

New series of thiophene derivatives were synthesized and evaluated for their in vivo anti-inflammatory activity using carrageenan-induced paw edema model. The most active in vivo anti-inflammatory compounds 5b, 11b, 14c, 18c, 19c and 20d were further evaluated for their in vitro COX-1/COX-2 and 5-LOX inhibitory activities. The in vitro assay results revealed that the N-(4-(4-chlorophenyl)-3-cyanothiophen-2-yl)-2-morpholinoacetamide (5b) possesses the highest selectivity toward COX-2 (IC50 = 5.45 μM) with selectivity index value of 8.37 compared to celecoxib with COX-2 selectivity index value of 15.44. In addition, it showed acceptable 5-LOX inhibitory activity (IC50 = 4.33 μM) compared to NDGA (IC50 = 2.46 μM). Molecular modeling study was conducted to study the postulated binding of compound 5b into the active site of COX-2 and 5-LOX, and it revealed that 5b binds similarly to celecoxib and NDGA, respectively. Overall, the morpholinoacetamide-thiophene hybrid 5b could serve as a promising lead for further development of new potent anti-inflammatory agents that act as dual COX-2/5-LOX inhibitors.

Ethylene diamine grafted nanoporous UiO-66 as an efficient basic catalyst in the multi-component synthesis of 2-aminithiophenes

This study demonstrates ED-UiO-66 as a novel and effective solid nanoporous basic catalyst prepared through the amine grafting onto the pores of UiO-66. The manufactured nanoparticles were identified by FT-IR, XRD, TGA, FESEM, TEM, CHN and BET and the characterization results certified formation of a single phase nanoporous substance with the medium grain size less than 90?nm. The synthesized material was employed as an efficient catalyst for the preparation of 2-aminotiophenes through the Gewald method. This thermochemically stable nanocatalyst was environmentally safe, reusable and economic. Therefore, this methodology can be simply extended for industrial goals.

Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d] pyrimidine or furo[2,3-d]pyrimidine scaffold

A series of thieno[2,3-d]pyrimidines and furo[2,3-d]pyrimidines were synthesized and evaluated for the c-Met inhibition. Thieno[2,3-d]pyrimidine 6b stood out as the most potent showing an IC50 of 35.7 nM. This compound displayed high inhibitory effect on cell proliferation in BaF3-TPR-Met cells and showed high selectivity for c-Met family against other 14 tested kinases. However, compound 6b was found ineffective in the c-Met-dependent U-87MG human gliobastoma xenograft model that may be relevant to its poor PK profile.

Novel thiophenes and analogues with anthelmintic activity against Haemonchus contortus

A new series of analogues of 4-(4-fluorophenyl)-2-methylthio-thiophene-3- carbonitrile (1) were synthesized and evaluated for their in vitro and in vivo anthelmintic activity against Haemonchus contortus.