Pyridine is a six-membered heterocyclic compound containing one nitrogen heteroatom. Pyridine and piperidine are the most frequently occurring heterocyclic building blocks in drug molecules. According to incomplete statistics, there are currently more than 180 drugs containing pyridine or piperidine structure that have been marketed, nearly 1/5 of the drugs approved for marketing in recent years contain these two structures.
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Pyridine is a basic heterocyclic organic compound with the chemical formula C5H5N. It is structurally related to benzene, with one methine group (=CH−) replaced by a nitrogen atom. It is a highly flammable, weakly alkaline, water-miscible liquid with a distinctive, unpleasant fish-like smell.
The Journal of Medicinal Chemistry recently publishes an article titled, “Discovery of Darovasertib, a Pan-PKC Inhibitor for the Treatment of Metastatic Uveal Melanoma”. Uveal melanoma (UM) is the most common primary intraocular malignancy. About half of primary uveal melanoma tumors metastasize but with no standard treatment. Most patients with metastatic uveal melanoma have been found to have mutations in GNAQ or GNA11, that are associated with consistent activation of the protein kinase C (PKC) and mitogen-activated protein kinase (MAPK) pathways.
IDEAYA's Darovasertib (IDE196) is a potent, selective small molecule inhibitor of PKC which stops activating PKC/MEK pathway. Darovasertib is under Phase 2 expansion and Phase 3 registrational trial with Crizotinib in GNAQ/11 metastatic cutaneous melanoma.
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