Discovery of 6-benzamide Containing 4-phenylquinazoline Derivatives as Novel PI3Kδ Inhibitors

Title:Discovery of 6-benzamide Containing 4-phenylquinazoline Derivatives as Novel PI3Kδ Inhibitors

Volume: 14 Issue: 2

Author(s): Minhang Xin, Yuan-Yuan Hei, Hao Zhang, Xiao-Xiao Xie, Shuai Mao, Sai-Jie Zuo and San-Qi Zhang

Affiliation:

Keywords: PI3Kδ inhibitors, 6-benzamide containing 4-phenylquinazoline, novel, SAR.

Abstract: In the present study, a series of new 6-benzamide containing 4-phenylquinazoline derivatives were designed and synthesized as PI3Kδ inhibitors. The preliminary SAR for this series of compounds was established. PI3Kδ inhibitory assay showed that most of the synthesized compounds achieved significant activity against PI3Kδ. Compound 12h was the most potent PI3Kδ inhibitor, displaying an IC₅₀ value of 17 nM. These results reveal that the 6-benzamide containing 4-phenylquinazoline is an encouraging chemical substructure, deserving further structural exploration to identify novel and highly potent PI3Kδ inhibitors.

Cite this article as:

Xin Minhang, Hei Yuan-Yuan, Zhang Hao, Xie Xiao-Xiao, Mao Shuai, Zuo Sai-Jie and Zhang San-Qi, Discovery of 6-benzamide Containing 4-phenylquinazoline Derivatives as Novel PI3Kδ Inhibitors, Letters in Drug Design & Discovery 2017; 14 (2) . https://dx.doi.org/10.2174/1570180813666160720160523