105807-79-2

Upstream product

• 85160-82-3 2-methyl-7-nitro-2-hydro-1,4-benzomorpholin-3-(4-hydro)-one 
• 121-88-0 5-Nitro-2-aminophenol 

Downstream Products

• 130137-57-4 1-(4-Bromo-phenyl)-3-(2-methyl-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-7-yl)-2-thioxo-dihydro-pyrimidine-4,6-dione 
• 130137-56-3 1-(4-Chloro-phenyl)-3-(2-methyl-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-7-yl)-2-thioxo-dihydro-pyrimidine-4,6-dione 
• 130137-55-2 1-(2-Methyl-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-7-yl)-3-phenyl-2-thioxo-dihydro-pyrimidine-4,6-dione 
• 130137-46-1 1-(4-Bromo-phenyl)-3-(2-methyl-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-7-yl)-thiourea 
• 130137-45-0 1-(4-Chloro-phenyl)-3-(2-methyl-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-7-yl)-thiourea 
• 130137-44-9 1-(2-Methyl-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-7-yl)-3-phenyl-thiourea 
• 105202-21-9 7-Amino-2-methyl-4H-benzo[1,4]oxazin-3-one; hydrochloride 

Relevant academic research and scientific papers

Synthesis and biological evaluation of N-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl)benzenesulfonamide derivatives as new BET bromodomain inhibitors for anti-hematologic malignancies activities

The bromodomain and extra-terminal proteins (BETs), in particular BRD4, has been reported to play important roles in cancer, inflammation, obesity, cardiovascular disease, and neurological disorders. In this paper, a series of benzomorpholinone derivatives were synthesized and biologically evaluated as BETs inhibitors. Detailed structure–activity relationship studies led to the discovery of several new potent compounds, of which 15h and 15i displayed IC 50 values of 2.8 and 4.5 μ M against BRD4 (D1), respectively, and showed good anti-proliferation activities against four hematologic malignancies cell lines at low-micromolar concentrations, including MV4-11, OCI-LY10, Pfeifer, and Su-DHL-6 cells. This chemotype could be further optimized with respect to its potency and drug-like properties in the future.

Benzomorpholone derivative as well as preparation method and application of benzomorpholone derivative

The invention belongs to the field of chemical medicines and particularly relates to a benzomorpholone derivative as well as a preparation method and application of the benzomorpholone derivative. The invention provides a benzomorpholone derivative with a structure as shown in the formula I and also provides a preparation method and application of the benzomorpholone derivative. The benzomorpholone derivative provided by the invention is novel in structure, has a good effect on selectively inhibiting BET targets, produces cytotoxicity for various tumor cells to different extents and is a novel BET small-molecule inhibitor. The compound disclosed by the invention has the potential to develop antitumor drugs.

Synthesis and Anthelmintic Activity of Some New 6- and 7-Isothiocyanato-2H-1,4-benzoxa(thia)zin-3(4H)-ones and Benzoxa(thia)zin-3(4H)-thiones

A series of 6- and 7-isothiocyanato-2H-1,4-benzoxa(thia)zin-3(4H)-ones (8a-n, 9a-c, 12a-i and 12l) and thiones (10a-h and 11a-c) has been prepared for anthelmintic testing.Some of these compounds possess a significant degree of activity against hookworm i