jnj-28312141 and Giant-Cell-Tumor-of-Tendon-Sheath

jnj-28312141 has been researched along with Giant-Cell-Tumor-of-Tendon-Sheath* in 1 studies

Other Studies

1 other study(ies) available for jnj-28312141 and Giant-Cell-Tumor-of-Tendon-Sheath

Article	Year
Discovery of vimseltinib (DCC-3014), a highly selective CSF1R switch-control kinase inhibitor, in clinical development for the treatment of Tenosynovial Giant Cell Tumor (TGCT). Bioorganic & medicinal chemistry letters, 2022, 10-15, Volume: 74 Based on knowledge of kinase switch-control inhibition and using a combination of structure-based drug design and standard medicinal chemistry principles, we identified a novel series of dihydropyrimidone-based CSF1R kinase inhibitors displaying exquisite selectivity for CSF1R versus a large panel of kinases and non-kinase protein targets. Starting with lead compound 3, an SAR optimization campaign led to the discovery of vimseltinib (DCC-3014; compound 20) currently undergoing clinical evaluation for the treatment of Tenosynovial Giant Cell Tumor (TGCT), a locally aggressive benign tumor associated with substantial morbidity. 2021 Elsevier ltd. All rights reserved. Topics: Antineoplastic Agents; DCC Receptor; Giant Cell Tumor of Tendon Sheath; Humans; Protein Kinase Inhibitors; Receptor Protein-Tyrosine Kinases; Receptor, Macrophage Colony-Stimulating Factor	2022

Article

Year

Discovery of vimseltinib (DCC-3014), a highly selective CSF1R switch-control kinase inhibitor, in clinical development for the treatment of Tenosynovial Giant Cell Tumor (TGCT).

Bioorganic & medicinal chemistry letters, 2022, 10-15, Volume: 74

Based on knowledge of kinase switch-control inhibition and using a combination of structure-based drug design and standard medicinal chemistry principles, we identified a novel series of dihydropyrimidone-based CSF1R kinase inhibitors displaying exquisite selectivity for CSF1R versus a large panel of kinases and non-kinase protein targets. Starting with lead compound 3, an SAR optimization campaign led to the discovery of vimseltinib (DCC-3014; compound 20) currently undergoing clinical evaluation for the treatment of Tenosynovial Giant Cell Tumor (TGCT), a locally aggressive benign tumor associated with substantial morbidity. 2021 Elsevier ltd. All rights reserved.

Topics: Antineoplastic Agents; DCC Receptor; Giant Cell Tumor of Tendon Sheath; Humans; Protein Kinase Inhibitors; Receptor Protein-Tyrosine Kinases; Receptor, Macrophage Colony-Stimulating Factor

2022