2. Academic Validation
  3. Synthesis and antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors

Synthesis and antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors

  • Bioorg Med Chem Lett. 2016 Sep 15;26(18):4408-4413. doi: 10.1016/j.bmcl.2016.08.015.
Yuan-Yuan Hei 1,  Minhang Xin 2,  Hao Zhang 1,  Xiao-Xiao Xie 1,  Shuai Mao 1,  San-Qi Zhang 3
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, School of Pharmacy, Xi'an Jiaotong University, Xi'an, Shaanxi 710061, PR China.
  • 2 Department of Medicinal Chemistry, School of Pharmacy, Xi'an Jiaotong University, Xi'an, Shaanxi 710061, PR China. Electronic address: xmhcpu@163.com.
  • 3 Department of Medicinal Chemistry, School of Pharmacy, Xi'an Jiaotong University, Xi'an, Shaanxi 710061, PR China. Electronic address: sqzhang@xjtu.edu.cn.
PMID: 27544401 DOI: 10.1016/j.bmcl.2016.08.015
Abstract

A series of 4,6-disubstituted quinazoline derivatives as potential PI3K inhibitors were designed and synthesized. All compounds exhibited significant anti-proliferative activities against HCT-116 and MCF-7 cell lines, and compounds A7, A9, and A11 displayed the most potent anti-proliferative activity against the HCT-116. Further PI3K inhibitory activity evaluation showed that compound A7 displayed high potency against PI3K Enzymes. The in vivo anti-tumor study showed compound A7 can efficaciously inhibit tumor growth in a mice S-180 model. These results suggest that our designed compounds can serve as potent PI3K inhibitors and effective antitumor agents.

Keywords

Anti-proliferative; Antitumor; PI3K inhibitor; Quinazoline derivatives; Synthesis.

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