Design and synthesis of novel pyrazolo[1,5-a]pyrimidine derivatives bearing nitrogen mustard moiety and evaluation of their antitumor activity in vitro and in vivo
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- 作者：Mingxia Zhaoa ; Hongyu Rena ; Jin Changa ; Diqin Zhanga ; Yating Yanga ; Yong Hea ; b ; Chuanmin Qia ; qicmin@sohu.com" class="auth_mail" title="E-mail the corresponding author ; Huabei Zhanga
- 关键词：Pyrazolo[1 ; 5-a]pyrimidine ; Nitrogen mustard derivatives ; Anti-tumor ; Cell cycle ; Apoptosis ; Xenograft mice model
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：25 August 2016
- 年：2016
- 卷：119
- 期：Complete
- 页码：183-196
- 全文大小：1726 K
文摘
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Pyrazolo[1,5-a]pyrimidines bearing nitrogen mustard moiety were prepared.
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Several compounds were more potent than the standard Sorafenib and Melphalan.
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13b could prevent the cell cycle progression and induce cell apoptosis.
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13b owned significant therapeutic efficacy in nude mice bearing HepG2 xenografts.