{Reference Type}: Journal Article
{Title}: Design and synthesis of novel thiazole-derivatives as potent ALK5 inhibitors.
{Author}: Arai M;Hanada M;Moriyama H;Ohmoto H;Miyake T;Naka K;Sawa M;
{Journal}: Bioorg Med Chem Lett
{Volume}: 108
{Issue}: 0
{Year}: 2024 Aug 1
{Factor}: 2.94
{DOI}: 10.1016/j.bmcl.2024.129797
{Abstract}: TGF-β is an immunosuppressive cytokine and plays a key role in progression of cancer by inducing immunosuppression in tumor microenvironment. Therefore, inhibition of TGF-β signaling pathway may provide a potential therapeutic intervention in treating cancers. Herein, we report the discovery of a series of novel thiazole derivatives as potent inhibitors of ALK5, a serine-threonine kinase which is responsible for TGF-β signal transduction. Compound 29b was identified as a potent inhibitor of ALK5 with an IC50 value of 3.7 nM with an excellent kinase selectivity.