67657-90-3

Upstream product

• 60541-89-1 5-bromo-2-methoxy-3-nitro-benzoic acid 
• 74-88-4 methyl iodide 
• 89-55-4 5-bromosalicyclic acid 
• 2476-35-9 5-bromo-2-methoxybenzoic acid 
• 77-78-1 dimethyl sulfate 

Downstream Products

• 1579281-63-2 methyl 3-(4-fluorophenylsulfonamino)-2-methoxy-5-(4-morpholinoquinazolin-6-yl)benzoate 
• 1404227-73-1 3-cyclopropylsulfonamino-2-methoxy-5-(4-morpholinoquinazolin-6-yl)benzamide 
• 1579281-58-5 methyl 5-bromo-2-methoxy-3-(4-fluorophenylsulfonamino)benzoate 
• 1404227-97-9 5-bromo-3-(cyclopropanesulfonylamino)-2-methoxybenzamide 
• 926069-76-3 3-amino-5-bromo-2-methoxy-benzoic acid methyl ester 

Relevant academic research and scientific papers

Discovery of 2-methoxy-3-phenylsulfonamino-5-(quinazolin-6-yl or quinolin-6-yl)benzamides as novel PI3K inhibitors and anticancer agents by bioisostere

2-Substituted-3-sulfonamino-5-(quinazolin-6-yl or quinolin-6-yl)benzamides have been proposed as novel structures of PI3K inhibitors and anticancer agents based on bioisostere. In the present study, 2-substituted-3-sulfonamino-5-(4- morpholinoquinazolin-6-yl)benzamides and 2-methoxy-3-sulfonamino-5-(4- morpholinoquinolin-6-yl)benzamides were synthesized. Their antiproliferative activities in vitro were evaluated via MTT assay against four human cancer cell lines, including A549, HCT-116, U-87 MG and KB. The SAR of the title compounds was preliminarily discussed. Compound 1a with potent antiproliferative activity was tested for its inhibitory activity against PI3K and mTOR and its effect on the AKT and p-AKT473. The anticancer effect of 1a was evaluated in established nude mice U-87 MG xenograft model. The results suggest that compound 1a can significantly inhibit PI3K/AKT/mTOR pathway and tumor growth. These findings strongly support the assumption that title compounds are potent PI3K inhibitors and anticancer agents.

Enforcing periodic secondary structures in hybrid peptides: A novel hybrid foldamer containing periodic γ-turn motifs

This note describes the design, synthesis, and conformational studies of a novel hybrid foldamer that adopts a definite compact, three-dimensional structure determined by a combined effect of the special conformational properties of the foldamer constituents. The striking feature of this de novo designed foldamer is its ability to display periodic γ-turn conformations stabilized by intramolecular hydrogen bonds. Conformational investigations by single-crystal X-ray studies, solution-state NMR, and ab initio MO theory at the HF/6-31G* level strongly support the prevalence of γ-turn motifs in both the di- and tetrapeptide foldamers, which are presumably stabilized by bifurcated hydrogen bonds in the solid and solution states. The strategy disclosed herein for the construction of hybrid foldamers with periodic γ-turn motifs has the potential to significantly augment the conformational space available for foldamer design with diverse backbone structures and conformations.