1258974-41-2

Upstream product

• 1258974-75-2 C₃₀H₃₈ClN₃O₄Si 
• 908567-28-2 C₁₁H₁₁BrO₃ 
• 89-84-9 2',4'-dihydroxy-4-acetophenone 
• 17771-33-4 7-hydroxy-2,2-dimethyl-chroman-4-one 
• 1354200-70-6 C₂₉H₃₁F₁₇O₂Si 
• 59068-43-8 4-(4-chlorophenyl)-1,2,4-triazoline-3,5-dione 
• 1354200-50-2 C₁₁H₁₁BrO₂ 
• 1354200-62-6 C₂₇H₂₈BrF₁₇O₂Si 
• 52039-87-9 4-(4-chlorophenyl)urazole 

Relevant academic research and scientific papers

Construction of polyheterocyclic benzopyran library with diverse core skeletons through diversity-oriented synthesis pathway: Part II

As a continuation of our previous report (J. Comb. Chem.2010, 12, 548-558), we accomplished the diversity-oriented synthesis of polyheterocyclic small-molecule library with privileged benzopyran substructure. To ensure the synthetic efficiency, we utilized the solid-phase parallel platform and the fluorous-tag-based solution-phase parallel platform to construct a 284-member polyheterocyclic library with six distinct core skeletons with an average purity of 87% on a scale of 5-10 mg. This library was designed to maximize the skeletal diversity with discrete core skeletons in three-dimensional space and the combinatorial diversity with four different benzopyranyl starting materials and various building blocks. Together with our reported benzopyranyl library, we completed the construction of polyheterocyclic benzopyran library with 11 unique scaffolds and their molecular diversity was visualized in chemical space using principle component analysis (PCA).

Discovery of novel benzopyranyl tetracycles that act as inhibitors of osteoclastogenesis induced by receptor activator of NF-κB ligand

A novel benzopyran-fused molecular framework 7ai was discovered as a specific inhibitor of RANKL-induced osteoclastogenesis using a cell-based TRAP activity assay from drug-like small-molecule libraries constructed by diversity-oriented synthesis. Its inhibitory activity was confirmed by in vitro evaluations including specific inhibition of RANKL-induced ERK phosphorylation and NF-κB transcriptional activation. 7ai can serve as a specific small-molecule modulator for mechanistic studies of RANKL-induced osteoclast differentiation as well as a potential lead for the development of antiresorptive drugs.