Soto, Sara; Vaz, Esther; Dell’Aversana, Carmela; Alvarez, Rosana; Altucci, Lucia; de Lera, Angel R. published an article in 2012, the title of the article was New synthetic approach to paullones and characterization of their SIRT1 inhibitory activity.Category: indole-building-block And the article contains the following content:
A series of 7,12-dihydroindolo[3,2-d][1]benzazepine-6(5H)-ones (paullones) substituted at C9/C10 (Br) and C2 (Me, CF3, CO2Me) have been synthesized by a one-pot Suzuki-Miyaura cross-coupling of an o-aminoarylboronic acid and Me 2-iodoindoleacetate followed by intramol. amide formation. Other approaches to the paullone scaffold based on Pd-catalyzed C-H activation were unsuccessful. In vitro enzymic assay with recombinant human SIRT-1 indicated a strong inhibitory profile for the series, in particular the analog with a methoxycarbonyl group at C2 and a bromine at C9. These compounds are, in general, inducers of granulocyte differentiation of the U937 acute leukemia cell line and cause a marked increase in pre-G1 of the cell cycle. The experimental process involved the reaction of Methyl 2-(6-bromo-1H-indol-3-yl)acetate(cas: 152213-63-3).Category: indole-building-block
The Article related to aminoarylboronic acid iodoindoleacetate suzuki amidation, Heterocyclic Compounds (One Hetero Atom): Higher-Membered Rings and other aspects.Category: indole-building-block
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Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles