876723-88-5

Upstream product

• 903161-06-8 ethyl 1-(2-oxo-2-phenylethyl)-1H-indole-2-carboxylate 
• 70-11-1 α-bromoacetophenone 
• 3770-50-1 2-carbethoxyindole 

Relevant academic research and scientific papers

Pyrrole- and indole-containing tranylcypromine derivatives as novel lysine-specific demethylase 1 inhibitors active on cancer cells

On the basis of previous research showing the capability of N-carbobenzyloxy-(Z-)amino acid-tranylcypromine (-TCPA) derivatives to inhibit LSD1, we inserted at the 4-amino-TCPA moiety first a Z-Pro (9) and a Z-Gly (10) residue and then, after the encouraging data obtained for 9, a pyrrole and an indole ring in which the relative N1 position carried a acetophenone, a N-phenyl/benzylacetamide, or a Z chain (11a-f and 12a-f, respectively). In both series, the Z-pyrrole and indole derivatives 11e, f and 12e, f displayed high LSD1 inhibitory activity. The compounds are able to inhibit LSD1 in NB4 cells, increasing the expression of two related genes, GFI-1b and ITGAM, and to induce cell growth arrest in the AML MB4-11 and APL NB4 cell lines. This journal is

Expedient synthesis of 6-aryl derivatives of 3,4-dihydro-1,4,4a,6a- tetraaza-benzo[a]fluoren-2-one: A new heterocyclic framework

3,4-Dihydro-1,4,4a,6a-tetraaza-benzo[a]fluoren-2-one, a new tetracyclic heterocyclic framework, is designed through a simple and convenient synthetic sequence. Its 6-aryl derivatives are synthesized starting from 1H-indole-2-carboxylic acid. The reaction of differently substituted phenacyl bromides with 1H-indole-2-carboxylic acid and POCl3-mediated cyclization of the resultant 1H-indole-2-carboxylic acid phenacyl ester provided 2-oxa-4a-aza-fluoren-1-one, and its sequential reaction with hydrazine and 2-chloro-acetamide furnished the desired new heterocyclic compounds 7a-f. Copyright Taylor & Francis Group, LLC.