Identification and characterization of novel indole based small molecules as anticancer agents through SIRT1 inhibition

Novel Indole‐Quinazolinone Based Amides as Cytotoxic Agents

“…The core indole‐2‐ester moiety 1a and 1b were prepared by the Fischer indole mechanism , a method mostly used for the synthesis of potentially interesting medicinal compounds. It comprises an aromatic C–H functionalization wherein N‐arylhydrazones are transformed into indoles efficiently . Then, the indole ring was N‐alkylated with methyl iodide (MeI) using potassium carbonate (K 2 CO 3 ) as a base at 0°C to affordethyl 5‐substituted‐1‐methyl‐1 H ‐indole‐2‐carboxylate, 2a and 2b .…”

“…It comprises an aromatic C–H functionalization wherein N‐arylhydrazones are transformed into indoles efficiently . Then, the indole ring was N‐alkylated with methyl iodide (MeI) using potassium carbonate (K 2 CO 3 ) as a base at 0°C to affordethyl 5‐substituted‐1‐methyl‐1 H ‐indole‐2‐carboxylate, 2a and 2b . A phase transfer catalyst, namely, tetra‐n‐butyl ammonium bromide (n‐TBAB) was used in the previous reaction, which accelerated the reaction process and improved the product yields as compared with our earlier method .…”

Facile synthesis of indole-pyrimidine hybrids and evaluation of their anticancer and antimicrobial activity

“…The core indole-2-ester (4a/4b) moiety was conveniently prepared using the Fischer-indole protocol [34]. The indole-NH was then methylated using potassium carbonate (K 2 CO 3 ) as base and tetra-n-butyl ammonium bromide (n-TBAB) as phase transfer catalyst to give intermediates 5a and 5b.…”

New indole–isoxazolone derivatives: Synthesis, characterisation and in vitro SIRT1 inhibition studies

“…All eighteen molecules contain a fluoro substitution at position-5 of indole ring. In our previous work, 18 we observed that the fluoro substitution contributes significantly to the inhibition activity of the molecules. So we selected 5-fluoro substituted indole scaffolds for the synthesis of indole-isoxazolone hybrids (I1-I18).…”

“…The basic indole-2-carboxylic ester (1) unit was synthesised by following Fischer indole synthetic protocol. 18 The ester intermediate was then subjected to three different synthetic routes to get the target compounds (I1-I18). In order to prepare the first set of compounds (I1-I9), the ester (1) was hydrolysed to get the corresponding carboxylic acid (2) which was then coupled with six different amines using EDCÁHCl and HOBt as the coupling agent to afford the corresponding amides (3a-f).…”