Structure activity relationship studies on Amb639752: toward the identification of a common pharmacophoric structure for DGKα inhibitors

• Main Authors: Suresh Velnati (Author), Alberto Massarotti (Author), Annamaria Antona (Author), Maria Talmon (Author), Luigia Grazia Fresu (Author), Alessandra Silvia Galetto (Author), Daniela Capello (Author), Alessandra Bertoni (Author), Valentina Mercalli (Author), Andrea Graziani (Author), Gian Cesare Tron (Author), Gianluca Baldanzi (Author)
• Format: Book
• Published: Taylor & Francis Group, 2020-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

A series of analogues of Amb639752, a novel diacylglycerol kinase (DGK) inhibitor recently discovered by us via virtual screening, have been tested. The compounds were evaluated as DGK inhibitors on α, θ, and ζ isoforms, and as antagonists on serotonin receptors. From these assays emerged two novel...