Given the putative role of PHGDH in cancer, development of inhibitors is
required to explore its function. In this context, we established and validated
a straightforward enzymatic assay suitable for high-throughput screening and we
identified inhibitors with similar chemical scaffolds. Through a convergent
pharmacophore approach, we synthesized α-ketothioamides
that exhibit interesting in vitro PHGDH inhibition and encouraging cellular
results. These novel probes may be used to understand the emerging biology of
this metabolic target.
Since 2011, a lot of quinazoline compounds have shown EGFR inhibition. Unlike the first-generation EGFR inhibitors, they inhibit both wild-type and mutated EGFR. In recent years, a number of studies on quinazoline synthesis have been reported and used by several medicinal chemistry groups for better and easier development of new derivatives. Therefore, several patents have been approved for the use of quinazoline compounds as inhibitors of other kinases, histone deacetylase, Nox and some metabolic pathways. Because of the large number of proteins targeted, some high structural diversity is observed in patented quinazoline compounds. Due to the vast applications of quinazoline derivatives, development of novel quinazoline compounds as anticancer drugs remains a promising field.
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