188107-70-2

Upstream product

• 74-83-9 methyl bromide 
• 14191-22-1 2-nitrocarbazole 
• 71857-97-1 2-acetamino-4'-nitro-1,1'-biphenyl 
• 171364-83-3 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)nitrobenzene 
• 614-76-6 N-acetyl-2-bromoaniline 
• 586-78-7 para-nitrophenyl bromide 
• 74-88-4 methyl iodide 
• 2486-04-6 2,4-dinitrobiphenyl 
• 584-48-5 2,4-dinitrobromobenzene 
• 86439-45-4 9-acetyl-2-nitro-9H-carbazole 
• 574-39-0 9-acetylcarbazole 

Downstream Products

• 86439-57-8 9-methyl-9H-carbazol-2-amine 

Relevant academic research and scientific papers

7-aminocarbazolesulfonamide derivatives as well as preparation method and application thereof

The invention provides 7-aminocarbazolesulfonamide derivatives as well as a preparation method and application thereof, and relates to the technical field of medicine. The 7-aminocarbazolesulfonamidederivatives have a general formula (I) shown in the description, wherein R1 is one or more groups located on a benzene ring and at least one independently selected from the group consisting of a C1-C6lower alkoxy group, a C1-C6 lower alkyl group, an amino group and a halogen; and R2 is hydrogen or a C1-C6 lower alkyl group. The 7-aminocarbazolesulfonamide derivatives provided by the invention exhibit good inhibitory activity against various tumor cells, so that the derivatives can be well used for preparing antitumor drugs.

Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubility

The current optimization of IG-105 (3) on the carbazole-ring provided a series of new carbazole sulfonamides derivatives 13a–13m. All of the compounds have been evaluated against HepG2 cells (hepatoma cancer) for antiproliferative activity. Compounds that showed activity better or comparable to that of 3 versus HepG2 were evaluated against MCF-7 (breast cancer), MIA PaCa-2 (pancreatic cancer), and Bel-7402 (hepatoma/liver cancer) for antiproliferative activity. Of the seven compounds selected for further study five (13b, 13g, 13j, 13k and 13l) were found to give IC50values against the four cell lines comparable to those for 3. Two compounds (13f and 13i) were more active than 3 and their activity against HepG2 and MCF-7 (IC50:0.01–0.07?μM) approached that of the positive controls podophyllotoxin (podo) and CA-4. Most of compounds showed aqueous solubility (0.11–19.60?μg/mL at pH 7.4 and 2.0) better than 3. These promising results warrant further development of new compounds 13f and 13i as potential potent antitumor drug candidates.

Lithiation of pivaloylamino derivatives of dibenzofuran and 9-methylcarbazole

2-, 3- and 4-Pivaloylamino derivatives of dibenzofuran [compounds (5), (4) and (6), respectively] and analogous 3-, 2- and 1-substituted derivatives of 9-methylcarbazole [compounds (8), (7) and (9), respectively] were subjected to lithiation at 0°C and subsequent reaction with dimethylformamide. Aldehyde formation took place at positions α to δ to the heteroatom as follows: α for (4) and (7); δ for (5); δ and β (3 : 1) for (8); and α′ (6). No formylation occurred with (9).