3258-15-9

Upstream product

• 98807-27-3 4-Methyl-benzoic acid (3aR,4R,6aR)-6-(4-hydroxy-2-oxo-2H-pyrimidin-1-yl)-2,2-dimethyl-tetrahydro-furo[3,4-d][1,3]dioxol-4-ylmethyl ester 
• 688007-27-4 [5-³H]uridine 
• 67-64-1 acetone 
• 55727-18-9 O^{2'_,O3'_{-isopropylidene-O}5'}-(4-oxo-pentanoyl)-uridine 

Relevant academic research and scientific papers

Design, synthesis, anticancer, antimicrobial activities and molecular docking studies of theophylline containing acetylenes and theophylline containing 1,2,3-triazoles with variant nucleoside derivatives

A new series of theophylline containing acetylene derivatives (6a–6b and 7–13) and theophylline containing 1,2,3-triazoles with variant nucleoside derivatives (20–32) have been designed and synthesized. These compounds were screened for anticancer and antimicrobial activity. Further the computational docking and 2D QSAR were performed using MOE software to identify novel scaffolds. The results showed that compound 29 and 30 exhibit significant cytotoxic effect on all four cancer cells such as lung (A549), colon (HT-29), breast (MCF-7) and melanoma (A375) with IC50values of 2.56, 2.19, 1.89, 4.89?μM and 3.57, 2.90, 2.10, 5.81?μM respectively. Whereas quite different results were observed for these compounds in antimicrobial studies. Compounds 11, 21 and 26 have exhibited significant minimum inhibitory concentrations (MIC) against Staphylococcus aureus, Bacillus cereus, Escherichia coli and Pseudomonas aeruginosa. The docking studies demonstrate that compound 27, 28, 29 and 30 have good dock score and binding affinities with various therapeutic targets in cancer cell proliferation. In addition these compounds have shown acceptable correlation with bioassay results in the regression plots generated in 2D QSAR models. This is the first report to demonstrate the theophylline containing acetylene derivatives and theophylline containing 1,2,3-triazole nucleoside hybrids as potential anticancer and antimicrobial agents with comprehensive in silico analysis.

A New Deprotection Method for Levulinyl Protecting Groups under Neutral Conditions

Sulfit ion-induced cleavage of the levulinyl group under neutral conditions provides a convenient and mild deprotection method especially for alkali labile and/or oxygen sensitive compounds.