Synthesis and anticancer activity of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives bearing chromone moiety
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- 作者：Chengyu Suna ; d ; &dagger ; ; Chen Chena ; &dagger ; ; Shan Xua ; Shanxu9891@126.com" class="auth_mail" title="E-mail the corresponding author ; Jianqiang Wangb ; Yan Zhuc ; Dejia Konga ; Hong Taoa ; Mengjia Jina ; Pengwu Zhenga ; Wufu Zhua ; zhuwufu-1122@163.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：Thiopyranopyrimidine ; Chromone ; Synthesis ; Docking ; mTOR ; PI3Kα ; Antitumor activity
- 刊名：Bioorganic & Medicinal Chemistry
- 出版年：2016
- 出版时间：15 August 2016
- 年：2016
- 卷：24
- 期：16
- 页码：3862-3869
- 全文大小：1037 K
文摘
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A series of 7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives bearing chromone moiety were designed and synthesized.
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Seven of the synthesized compounds showed moderate to significant antitumor activity.
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6-COOH substitution of chromone moiety produced the best potency.
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Compound 10j was more active than compound II.
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Docking study was investigated to explore the binding modes of compounds with mTOR and PI3Kα.