210426-42-9

Upstream product

• 174367-69-2 1-[(3-bromophenyl)methyl]-1H-indole-3-carboxaldehyde 
• 487-89-8 Indole-3-carboxaldehyde 
• 823-78-9 meta-bromobenzyl bromide 

Downstream Products

• 261637-59-6 bis[1-[(3-bromophenyl)methyl]-1H-indole-3-]methane 

Relevant academic research and scientific papers

Analogues and derivatives of oncrasin-1, a novel inhibitor of the C-terminal domain of RNA polymerase II and their antitumor activities

To optimize the antitumor activity of oncrasin-1, a small molecule RNA polymerase II inhibitor, we evaluated 69 oncrasin-1 analogues for their cytotoxic activity against normal human epithelial cells and K-Ras mutant tumor cells. About 40 of those compoun

Synthesis of trifluoromethylindolocarbazoles, novel cyclic 18-membered and 27-membered N-arylmethyldi- and triindoles and an N-arylmethyltetraindolyltrimethane

5,11-Dihydro-5,11-diarylmethyl-6-trifluoromethylindolo[3,2-b]carbazoles (3b-d) have been synthesised from both N-arylmethylindole-3-carbinols (1b-d) and N,N′-diarylmethyl-3,3′-diindolylmethanes (2b, c and f) by treatment with trifluoroacetic anhydride. The cyclic N-arylmethylindoledi- and trimers (4c-f) and the 3-trifluoroacetylindoles (5a and b) have also been obtained from this reaction. Thermal reaction of 1b-d furnishes 2b, c and f, but 1c also affords the N-arylmethyltriindolyldimethane (2d) and the N-arylmethyltetraindolyltrimethane (2e). The results are discussed and the plausible reaction mechanism is very briefly presented.

3-(Azolylmethyl)-1H-indoles as selective P450 aromatase inhibitors

The synthesis of 1-(halobenzyl) and 1-tosyl-3-(1H-imidazol-1-ylmethyl)-1H-indoles, 1-(halobenzyl) and 1-tosyl-3-(1H-1,2,4-triazol-1-ylmethyl)-1H-indoles and 1-(halobenzyl)-3-(4H-1,2,4-triazol-4-ylmethyl)-1H-indoles is described. 3-(Azolylmethyl)-1H-indoles were obtained in three steps from 1H-indole-3-carbaldehyde (1) by benzylation or tosylation, reduction and azole moiety fixation. In an alternative method, the bromo intermediates issued from the corresponding alcohols were condensed with the azolium sodium salts. Inhibitory activity against P450(arom) and P450(17α), and influence on retinoic acid metabolism were evaluated. Three imidazole compounds exhibited potent and selective aromatase inhibitory activity.