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

Autor: Veale, Clinton G L, Edkins, Adrienne Lesley, De la Mare, Jo-Anne, De Kock, Carmen, Smith, Peter J, Khanye, Setshaba D
Jazyk: angličtina
Rok vydání: 2015
Druh dokumentu: Článek
DOI: 10.1016/j.tetlet.2015.02.090
Popis: publisher version
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.
Databáze: Networked Digital Library of Theses & Dissertations