1421933-32-5

Upstream product

• 131645-73-3 2-amino-3-nitrobenzoyl chloride 
• 606-18-8 3-nitroanthranilic acid 
• 455-14-1 4-trifluoromethylphenylamine 
• 1622400-50-3 2-amino-N-(4-(trifluoromethyl)phenyl)-3-nitrobenzamide 

Downstream Products

• 1622400-84-3 N-(4-(trifluoromethyl)phenyl)-3-(1-(benzylamino)-2-methyl-1-oxopropan-2-yl)-2,4-dioxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepine-6-carboxamide 

Relevant academic research and scientific papers

Design, synthesis and inhibitory activity against human dihydroorotate dehydrogenase (hDHODH) of 1,3-benzoazole derivatives bearing amide units

A series of 1,3-benzoazole derivatives possessing amide moieties were designed, synthesized and evaluated as inhibitors against human dihydroorotate dehydrogenase (hDHODH). Compounds A11, A14 and A26 exhibited good to excellent activities against hDHODH at the concentration of 10 μM. In particular, compound A14 displayed an IC50 value of 0.178 μM with 2-fold preference over A771726. The result implied that a proper degree of steric size and electron density of the C-6 amide moiety was necessary to retain the inhibitory activity of the synthesized compounds.

Discovery of novel 1,5-benzodiazepine-2,4-dione derivatives as potential anticancer agents

A series of novel 1,5-benzodiazepine-2,4-dione derivatives with C-6 amide substituents were designed and synthesized using three-component reactions. The preliminary assays showed that most of them displayed moderate to good antitumor activities against human lung carcinoma (A549), human breast epithelial carcinoma (MCF-7), human colon carcinoma (HCT116), human cervical carcinoma (Hela) and Lewis lung carcinoma (2LL). Exhilaratingly, the activity level of 6m rivaled that of 5-Fluorouracil (5-Fu) against MCF-7 cell lines, which might be used as novel lead scaffold for potential anticancer development.