1031968-93-0

Upstream product

• 23903-46-0 ethyl 2-amino-3-cyano-4-methylthiophene-5-carboxylate 
• 832113-96-9 methyl 4-chloro-5-methylthieno[2,3-d]pyrimidine-6-carboxylate 
• 371-40-4 4-fluoroaniline 
• 350-46-9 4-Fluoronitrobenzene 

Downstream Products

• 1416273-82-9 C₂₁H₁₄FN₅OS 
• 1416273-83-0 C₂₁H₁₃ClFN₅OS 
• 1416273-84-1 C₂₁H₁₃FN₆O₃S 

Relevant academic research and scientific papers

An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis

Deregulation of protein synthesis is a common event in cancer. As MAPK-interacting kinases (Mnks) play critical roles in regulation of protein synthesis, they have emerged as novel anti-cancer targets. Mnks phosphorylate eukaryotic initiation factor 4E (eIF4E) and promote eIF4E-mediated oncogenic activity. Given that the kinase activity of Mnks is essential for oncogenesis but is dispensable for normal development, the discovery of potent and selective pharmacological Mnk inhibitors provides pharmacological target validation and offers a new strategy for cancer treatment. Herein, comprehensive in silico screening approaches were deployed, and three thieno[2,3-d]pyrimidine and pyrazolo[3,4-d]pyrimidine derivatives were identified as hit compounds. Further chemical modification of thieno[2,3-d]pyrimidine derivative 3 has given rise to a series of highly potent Mnk2 inhibitors that could be potential leads for the treatment of acute myeloid leukemia.

Synthesis and antioxidant activity of 1,3,4-oxadiazole tagged thieno[2,3-d]pyrimidine derivatives

This study represents the synthesis of a new series of N-substituted phenyl-5-methyl-6-(5-(4-substituted phenyl)-1,3,4-oxadiazol-2-yl)thieno[2,3-d] pyrimidin-4-amine derivatives (4a-l) and substituted phenylamino-5- methylthieno[2,3-d]pyrimidine-6-carboxylic acid derivatives (3a-d). The newly synthesized compounds were characterized by 1H NMR, 13C NMR, LC-MS and IR analyses. All these novel compounds were screened for their in vitro antioxidant activity by employing DPPH, hydrogen peroxide, and nitric oxide radical scavenging assays. Compounds 4k, 4j, 4d, and 4e showed significant radical scavenging due to the presence of electron donating substituent on both sides of the thienopyrimidine ring enhances the activity and electron withdrawing groups like nitro decrease.