4750-22-5

Upstream product

• 577-19-5 2-nitrophenyl bromide 
• 98-58-8 4-bromobenzenesulfonyl chloride 

Downstream Products

• 1604061-33-7 phenyl 4-bromo-3-nitrobenzenesulfonate 
• 1604061-34-8 phenyl 3-nitro-4-(thiophen-3-yl)benzenesulfonate 
• 1604062-54-5 4-(methyl(phenyl)amino)-3-nitro-N-phenylbenzenesulfonamide 
• 4750-20-3 3-nitro-4-bromobenzenesulfonamide 
• 1604059-88-2 N-cyclopropyl-3-nitro-4-(thiophen-3-yl)benzenesulfonamide 
• 1604060-07-2 3-amono-N-cyclopropyl-4-(thiophen-3-yl)benzenesulfonamide 

Relevant academic research and scientific papers

Design and synthesis of novel 2-arylbenzimidazoles as selective mutant isocitrate dehydrogenase 2 R140Q inhibitors

A series of novel 2-arylbenzimidazoles have been designed, synthesized and evaluated for their inhibitory activity against IDH2 R140Q mutant. The preliminary results indicated that four compounds 7b, 7c, 7m and 7r displayed the potent inhibitory activity against IDH2 R140Q mutant. Among them, compound 7c showed the highest inhibitory activity, with the IC50 value of 0.26 μM, which was more active than positive control enasidenib. The exquisite selectivity of 7c for IDH2 R140Q mutant isoform was demonstrated by the poor activity against the IDH1 R132C mutant, IDH1 R132H mutant, wild-type IDH1, IDH2 R172K mutant and the wild-type IDH2.

Benzenesulfonamide IDH mutant inhibitor, preparation method and application thereof

The invention discloses a benzenesulfonamide compound represented by a general formula (I) or a pharmaceutically acceptable salt thereof, a preparation method and application thereof. Compared with the prior art, the benzenesulfonamide compound disclosed by the invention can be used as an isocitrate dehydrogenase 2 (IDH2) mutant inhibitor. According to the invention, pharmacological experiment results show that the compound disclosed by the invention has an obvious inhibiting effect on the activity of an IDH2 mutant (mIDH2), can effectively inhibit the process of catalyzing alpha-ketoglutaricacid to generate 2-hydroxyglutaric acid by mIDH2, and can be used for preventing and/or treating various related diseases including cancers and the like caused by IDH2 mutation.

Amplified synthesis method of 3-nitro-4-halogeno-benzenesulfonamide

An amplified synthesis method of 3-nitro-4-halogeno-benzenesulfonamide is disclosed. According to the method, 4-halogeno-benzenesulfonyl chloride which is used as a raw material undergoes nitration to prepare 3-nitro-4-halogeno-benzenesulfonyl chloride; and after aminolysis, 3-nitro-4-halogeno-benzenesulfonamide is prepared. By the synthesis method provided by the invention, the synthesis route by the adoption of chlorosulfonic acid is changed, and production safety is remarkably raised. The reaction condition is milder and is easy for production control. Thus, mass production of the compound is easier to implement and realize.

THERAPEUTIC COMPOUNDS AND COMPOSITIONS

Provided are aryl sulfonamide diarylurea derivative compounds that are inhibitors of mutant isocitrate dehydrogenase 1/2 (IDH 1/2), useful for treating cancer. Also provided are methods of treating cancer comprising administering to a subject in need thereof a compound described herein. Cancers that are treatable by the compounds of the invention are glioblastoma, myelodysplastic syndrome, myeloproliferative neoplasm, acute myelogenous leukemia, sarcoma, melanoma, non-small cell lung cancer, chondrosarcoma, and non-Hodgkin's lymphoma (NHL).