Design and Synthesis of Novel Quinazoline Derivatives and Their Evaluation as PI3Ks Inhibitors
-
- 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
Bibliographic Information
- Other Title
-
- Communication to the Editor : Design and Synthesis of Novel Quinazoline Derivatives and Their Evaluation as PI3Ks Inhibitors
Search this article
Abstract
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.
Journal
-
- Chemical and Pharmaceutical Bulletin
-
Chemical and Pharmaceutical Bulletin 62 (12), 1166-1172, 2014
The Pharmaceutical Society of Japan
- Tweet
Keywords
Details 詳細情報について
-
- CRID
- 1390282679153624832
-
- NII Article ID
- 130004712918
-
- NII Book ID
- AA00602100
-
- ISSN
- 13475223
- 00092363
-
- NDL BIB ID
- 025935934
-
- PubMed
- 25450624
-
- Text Lang
- en
-
- Data Source
-
- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
-
- Abstract License Flag
- Disallowed