213554-28-0

Upstream product

• 39824-26-5 6-chloro-9-(2,3-O-isopropylidene-β-D-ribofuranosyl)-9H-purine 
• 2004-06-0 6-Chloropurine riboside 

Downstream Products

• 1310342-91-6 ((3aR,4R,6R,6aR)-2,2-dimethyl-6-(6-(phenylamino)-9H-purin-9-yl)tetrahydrofuro[3,4-d][1,3]dioxol-4-yl)methyl sulfamate 
• 1310342-20-1 ((2R,3S,4R,5R)-3,4-dihydroxy-5-(6-(phenylamino)-9H-purin-9-yl)tetrahydrofuran-2-yl)methyl sulfamate 

Relevant academic research and scientific papers

Synthesis and biological evaluation of lipophilic nucleoside analogues as inhibitors of aminoacyl-tRNA synthetases

Emerging antibiotic resistance in pathogenic bacteria and reduction of compounds in the existing antibiotics discovery pipeline is the most critical concern for healthcare professionals. A potential solution aims to explore new or existing targets/compoun

Identification of NAE inhibitors exhibiting potent activity in leukemia cells: Exploring the structural determinants of NAE specificity

MLN4924 is a selective inhibitor of the NEDD8-activating enzyme (NAE) and has advanced into clinical trials for the treatment of both solid and hematological malignancies. In contrast, the structurally similar compound 1 (developed by Millennium: The Takeda Oncology Company) is a pan inhibitor of the E1 enzymes NAE, ubiquitin activating enzyme (UAE), and SUMO-activating enzyme (SAE) and is currently viewed as unsuitable for clinical use given its broad spectrum of E1 inhibition. Here, we sought to understand the determinants of NAE selectivity. A series of compound 1 analogues were synthesized through iterative functionalization of the purine C6 position and evaluated for NAE specificity. Optimal NAE specificity was achieved through substitution with primary N-alkyl groups, while bulky or secondary N-alkyl substituents were poorly tolerated. When assessed in vitro, inhibitors reduced the growth and viability of malignant K562 leukemia cells. Through this study, we have successfully identified a series of sub-10 nM NAE-specific inhibitors and thereby highlighted the functionalities that promote NAE selectivity.

Aminoacyl sulfamides for the treatment of hyperproliferative disorders

Novel aminoacyl sulfamides are described. These compounds are effective in the treatment of hyperproliferative disorders, specifically psoriasis. Exemplary compounds of this invention are 5'-deoxy-adenosine 5'-N(N-L-phenylalanyl)sulfamide and 5'-deoxy-ade