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Title: Triazolopyrimidinium salts: discovery of a new class of agents for cancer therapy
Authors: Badolato, Mariateresa
Manetti, Fabrizio 
Garofalo, Antonio
Aiello, Francesca
Keywords: 1,2,4-triazolo-[1,5-a]pyrimidinium salts; SH2 domain; STAT3 inhibition; STAT3 protein; anticancer agents; antiproliferative activity; binding assay; cell colony formation; chemotherapeutics; docking simulation; fluorescence polarization assay; privileged scaffold; purine analogs
Issue Date: 2020
Project: None 
Aim: The [1,2,4]triazolo[1,5-a]pyrimidine core is highly privileged in medicinal chemistry due to its versatile pharmacological activity profile. Recently, the search for novel anticancer agents has focused on [1,2,4]triazolo[1,5-a]pyrimidine derivatives. Results: Our hit functionalization has led to the discovery of new [1,2,4]triazolo[1,5-a]pyrimidinium salts with potential anticancer activity. Among a small library of molecules, compound 9 significantly inhibits cancer cell growth in a panel of in vitro models. Molecular docking studies and preliminary binding assay have displayed that 9 could directly bind the Src homology 2 (SH2) domain of STAT3 protein. Conclusion: Compound 9 is a novel promising lead compound that motivates additional evaluation of [1,2,4]triazolo[1,5-a]pyrimidinium salts as novel potential chemotherapeutics.
ISSN: 1756-8919
DOI: 10.4155/fmc-2019-0317
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