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|Title:||Triazolopyrimidinium salts: discovery of a new class of agents for cancer therapy||Authors:||Badolato, Mariateresa
|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||Journal:||FUTURE MEDICINAL CHEMISTRY||Abstract:||
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.
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