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

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• 作者：Yuan-Yuan Hei ; Minhang Xin ; ^{xmhcpu@163.com" class="auth_mail" title="E-mail the corresponding author} ; Hao Zhang ; Xiao-Xiao Xie ; Shuai Mao ; San-Qi Zhang ; ^{sqzhang@xjtu.edu.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Quinazoline derivatives ; Synthesis ; Anti-proliferative ; PI3K inhibitor ; Antitumor
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 September 2016
• 年：2016
• 卷：26
• 期：18
• 页码：4408-4413
• 全文大小：3171 K

文摘

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.