Facile synthesis and biological evaluation of assorted indolyl-3-amides and esters from a single, stable carbonyl nitrile intermediate

Veale, Clinton G L; Edkins, Adrienne L; de la Mare, Jo-Anne; de Kock, Carmen; Smith, Peter J; Khanye, Setshaba D

Title: Facile synthesis and biological evaluation of assorted indolyl-3-amides and esters from a single, stable carbonyl nitrile intermediate
Creator: Veale, Clinton G L
Creator: Edkins, Adrienne L
Creator: de la Mare, Jo-Anne
Creator: de Kock, Carmen
Creator: Smith, Peter J
Creator: Khanye, Setshaba D
Date Issued: 2015
Date: 2015
Type: text
Type: article
Identifier: http://hdl.handle.net/10962/66221
Identifier: vital:28919
Identifier: https://doi.org/10.1016/j.tetlet.2015.02.090
Description: publisher version
Description: The synthesis of biologically relevant amides and esters is routinely conducted under complex reaction conditions or requires the use of additional catalysts in order to generate sensitive electrophilic species for attack by a nucleophile. Here we present the synthesis of different indolic esters and amides from indolyl-3-carbonyl nitrile, without the requirement of anhydrous reaction conditions or catalysts. Additionally, we screened these compounds for potential in vitro antimalarial and anticancer activity, revealing 1H-indolyl-3-carboxylic acid 3-(indolyl-3-carboxamide)aminobenzyl ester to have moderate activity against both lines.
Format: 5 pages
Format: pdf
Language: English
Relation: Tetrahedron Letters
Relation: Veale, Clinton G.L., Edkins, Adrienne L., De la Mare, Jo-Anne, De Kock, Carmen, Smith, Peter J., Khanye, Setshaba D. (2015) Facile synthesis and biological evaluation of assorted indolyl-3-amides and esters from a single, stable carbonyl nitrile intermediate. Tetrahedon Letters, 56 (14), p. 1860-1864. SN-0040-4039. https://doi.org/10.1016/j.tetlet.2015.02.090
Relation: Tetrahedron Letters volume 56 number 14 1860 1864 April 2015 0040-4039
Rights: Elsevier B.V.
Rights: Use of this resource is governed by the terms and conditions of the Tetrahedron Letters Open Access Options Statement (https://www.elsevier.com/journals/tetrahedron-letters/0040-4039/open-access-options)

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RU DST/NRF SARChI for Molecular and Cellular Biology of the Eukaryotic Stress Response

De la Mare, Jo-Anne (Dr)

Veale, Clinton G L (Dr)

Khanye, David Setshaba (Associate Prof)

RU Department of Chemistry

RU Department of Pharmacy

SDG 03. Good Health and Well-Being

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