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ID: ALA3600296
Journal: Bioorg Med Chem Lett
Title: Synthesis and evaluation of pyrrolotriazine based molecules as PI3 kinase inhibitors.
Authors: Dugar S, Hollinger FP, Kuila B, Arora R, Sen S, Mahajan D.
Abstract: Over activation of the PI3K/Akt/mTOR pathway is found in most cancer tumor types. Controlled regulation of this pathway using PI3K inhibitors can provide therapeutic significance in cancer treatment. Herein, we report the synthesis and evaluation of pyrrolotriazine based novel small molecules as pan-PI3K inhibitors. The SAR studies based on in vitro potency along with microsomal metabolic stability screening, identified 18 as a preclinical lead found to be suitable for in vivo evaluation. The identified lead was also found to be a selective inhibitor of PI3K isoforms and mTOR when screened across a panel of 23 homologous kinases.
CiteXplore: 26112437