1082169-75-2

Upstream product

• 101667-98-5 5-Methyl-4-chloro-6-ethoxycarbonylthieno<2,3-d>pyrimidine 
• 17417-67-3 3,4-Dihydro-5-methyl-4-oxothieno<2,3-d>pyrimidin-6-carbonsaeure-ethylester 
• 4815-30-9 diethyl 5-amino-3-methyl-2,4-thiophenedicarboxylate 
• 113417-54-2 ethyl 4–(4-chlorophenylamino)-5-methylthieno[2,3-d]pyrimidine-6-carboxylate 
• 106-47-8 4-chloro-aniline 
• 23903-46-0 ethyl 2-amino-3-cyano-4-methylthiophene-5-carboxylate 

Downstream Products

• 1416273-79-4 C₂₁H₁₄ClN₅OS 
• 1416273-80-7 C₂₁H₁₃Cl₂N₅OS 
• 1416273-81-8 C₂₁H₁₃ClN₆O₃S 

Relevant academic research and scientific papers

Molecular design, synthesis and in vitro biological evaluation of thienopyrimidine–hydroxamic acids as chimeric kinase HDAC inhibitors: a challenging approach to combat cancer

A series of thieno[2,3-d]pyrimidine-based hydroxamic acid hybrids was designed and synthesised as multitarget anti-cancer agents, through incorporating the pharmacophore of EGFR, VEGFR2 into the inhibitory functionality of HDAC6. Three compounds (12c, 15b and 20b) were promising hits, whereas (12c) exhibited potent VEGFR2 inhibition (IC50=185 nM), potent EGFR inhibition (IC50=1.14 μM), and mild HDAC6 inhibition (23% inhibition). Moreover, compound (15c) was the most potent dual inhibitor among all the synthesised compounds, as it exhibited potent EGFR and VEGFR2 inhibition (IC50=19 nM) and (IC50=5.58 μM), respectively. While compounds (20d) and (7c) displayed nanomolar selective kinase inhibition with EGFR IC50= 68 nM and VEGFR2 IC50= 191 nM, respectively. All of the synthesised compounds were screened in vitro for their cytotoxic effect on 60 human NCI tumour cell lines. Additionally, molecular docking studies and ADMET studies were carried out to gain further insight into their binding mode and predict the pharmacokinetic properties of all the synthesised inhibitors.

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.