Related Products of 2343-22-8. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 5-Fluoroindoline, is researched, Molecular C8H8FN, CAS is 2343-22-8, about Discovery and Optimization of Pyrimidone Indoline Amide PI3Kβ Inhibitors for the Treatment of Phosphatase and Tensin Homologue (PTEN)-Deficient Cancers.
Compelling mol. biol. publications have reported the implication of phosphoinositide kinase PI3Kβ in PTEN-deficient cell line growth and proliferation. These findings supported a scientific rationale for the development of PI3Kβ-specific inhibitors for the treatment of PTEN-deficient cancers. This paper describes the discovery of 2-[2-(2,3-dihydro-indol-1-yl)-2-oxo-ethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one and the optimization of this new series of active and selective pyrimidone indoline amide PI3Kβ inhibitors. 2-[2-(2-Methyl-2,3-dihydro-indol-1-yl)-2-oxo-ethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one (I), identified following a carefully designed Me scan, displayed improved physicochem. and in vitro pharmacokinetic properties. Structural biol. efforts enabled the acquisition of the first x-ray cocrystal structure of p110β with the selective inhibitor compound I bound to the ATP site. The nonplanar binding mode described herein is consistent with observed structure-activity relationship for the series. Compound I demonstrated significant in vivo activity in a UACC-62 xenograft model in mice, warranting further preclin. investigation. Following successful development, compound 28 entered phase I/Ib clin. trial in patients with advanced cancer.
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Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics