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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Titolo: | Triazolopyrimidinium salts: discovery of a new class of agents for cancer therapy |
Autori: | AIELLO, Francesca (Corresponding) |
Data di pubblicazione: | 2020 |
Rivista: | |
Handle: | http://hdl.handle.net/20.500.11770/301863 |
Appare nelle tipologie: | 1.1 Articolo in rivista |