Communication to the Editor : Design and Synthesis of Novel Quinazoline Derivatives and Their Evaluation as PI3Ks Inhibitors

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  • El-Said Omar Maged
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Biotechnology, German University in Cairo
  • Hamed Mostafa Mohamed
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Biotechnology, German University in Cairo Helmholz Institute for Pharmaceutical Research, Saarland University
  • Laufer Stefan
    Department of Pharmaceutical & Medicinal Chemistry, Institute of Pharmacy, Eberhard-Karls-University Tuebingen
  • Abadi Ashraf Hassan
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Biotechnology, German University in Cairo

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  • Design and Synthesis of Novel Quinazoline Derivatives and Their Evaluation as PI3Ks Inhibitors

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The aim of this work was to synthesize 4-acetamido-, 4-amino- and 4-oxo-6-substituted aminoquinazolines and to evaluate them as phosphoinositide 3-kinases (PI3Ks) inhibitors. The respective chemotype was designed based on combining the structural features of two previously reported scaffolds acting as potent PI3Kγ inhibitors, which are quinazoline derivatives and amino-heterocyclic derivatives. In vitro enzymatic assay at 10 µM against all the eight human PI3K isoforms showed that an unsubstituted benzamide group at position 6 and an acetyl group at N4 gave the best inhibitory activity on PI3Kγ. Interestingly, compounds 5a and 5e showed a significant, inhibitory effect on Class II PI3K-C2γ. This is of high value since there are very few inhibitors for this isoform reported in the literature.

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