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Upstream product

• 6313-54-8 2-chloroisonicotinic acid, 
• 70696-29-6 2-chloroisonicotinoyl azide 
• 14432-12-3 4-Amino-2-chloropyridine 
• 32315-10-9 bis(trichloromethyl) carbonate 

Relevant academic research and scientific papers

Identity, Synthesis, and Cytotoxicity of Forchlorfenuron Metabolites in Kiwifruit

Forchlorfenuron (CPPU) is a plant growth regulator widely used in kiwifruit production. Although research on the toxicological and environmental effects of CPPU is well-established, the nature and toxicological properties of its metabolites are much less well-known. Using high resolution mass spectrometry and nuclear magnetic resonance, the CPPU previously unidentified metabolites in Xuxiang and Jinyan kiwifruit were identified as N-(2-chloro-4-pyridinyl)-N′-(2-hydroxy-4-methoxyphenyl)-urea (metabolite 1) and N-phenyl-N′-4-pyridinylurea (metabolite 2, CAS: 1932-35-0). Their structures were confirmed by synthesis (metabolite 1) and by comparison with a commercial standard (metabolite 2). Quantitative studies demonstrate that CPPU and its metabolites are mainly retained in the kiwifruit peel, while the content is dependent on the nature of the peel surface, with the smoother peel of Jinyan kiwifruit retaining smaller amounts of the compound. Cell viability experiments in Caco2 and Lo2 cells show that the metabolites may have a lower cytotoxicity compared to the parent compound CPPU.

S1PR2 inhibitors potently reverse 5-FU resistance by downregulating DPD expression in colorectal cancer

In this study, S1PR2 was reckoned as a brand-new GPCR target for designing inhibitors to reverse 5-FU resistance. Herein a series of pyrrolidine pyrazoles as the S1PR2 inhibitors were designed, synthesized and evaluated for their activities of anti-FU-resistance. Among them, the most promising compound JTE-013, exhibited excellent inhibition on DPD expression and potent anti-FU-resistance activity in various human cancer cell lines, along with the in vivo HCT116DPD cells xenograft model, in which the inhibition rate of 5-FU was greatly increased from 13.01percent–75.87percent. The underlying mechanism was uncovered that JTE-013 demonstrated an anti-FU-resistance activity by blocking S1PR2 internalization to the endoplasmic reticulum (ER), which inhibited the degradation of 5-FU into α-fluoro-β-alanine (FBAL) by downregulating tumoral DPD expression. Overall, JTE-013 could serve as the lead compound for the discovery of new anti-FU-resistance drugs. Significance: This study provides novel insights that S1PR2 inhibitors could sensitize 5-FU therapy in colorectal cancer.

4-Aminopyridine derivatives with anticholinesterase and antiamnesic activity

Several carbamate derivatives of 4-aminopyridine were synthesized and their anticholinesterase activity was evaluated. Compound 4d showed the highest inhibitory effect blocking non-competitively acetylcholinesterase and competitively butyrylcholinesterase

PYRIDINE DERIVATIVES AND USE THEREOF AS UROTENSIN II ANTAGONISTS

The invention relates to novel pyridine derivatives of formula 1 and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and their use as neurohormonal antagonists, especially as urotensin II inhibitors.