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DOI: 10.1055/a-2698-3056
Three-Step Synthesis of 3-Aminoindole-2-carboxylate-Conjugated 2-Amino-6-chloropyrimidines and Their Anticancer Activity
We would like to thank the Council of Scientific and Industrial Research, India (CSIR) for financial assistance from the Agromission projects (HCP-0049). A.N.P. would like to thank the Department of Science and Technology, Ministry of Science and Technology, India (DST-INSPIRE) for a fellowship program providing funding for this project (IF180770).
Abstract
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-benzonitriles and 2-aminopyrimidine-glycinates, culminating in the formation of 2-aminopyrimidine-indole hybrids. Biological evaluation of the products against three human cancer cell lines and one normal cell line revealed moderate anticancer activity and minimal toxicity, highlighting their potential as promising leads for further anticancer drug development.
Supporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/a-2698-3056.
- Supporting Information
Publication History
Received: 04 July 2025
Accepted after revision: 09 September 2025
Accepted Manuscript online:
09 September 2025
Article published online:
23 September 2025
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