Three-Step Synthesis of 3-AminoIndole-2-carboxylate conjugated 2-Amino-6-chloropyrimidines and Their Anticancer Activity

The synthesis of novel indolo-pyrimidine derivatives is of considerable interest due to the combined pharmacological benefits of indole and pyrimidine cores, particularly for anticancer applications. In this study, we report an efficient three-step synthesis of a novel series of 3-amino-1-(2-amino-6-chloropyrimidin-4-yl)-1H-indole-2-carboxylate derivatives, employing specific bases and solvents, in high yields. The synthetic route proceeds through key intermediates—2-aminopyrimidine-benzonitrile and 2-aminopyrimidine-glycinate culminating in the formation of 2-aminopyrimidine-indole hybrids. Biological evaluation against three human cancer cell lines and one normal cell line demonstrated moderate anticancer activity and minimal toxicity, highlighting their potential as promising leads for further anticancer drug development.

Publikationsverlauf

Eingereicht: 04. Juli 2025

Angenommen nach Revision: 09. September 2025

Accepted Manuscript online:
09. September 2025