Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs

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• 作者：Songwen Lin¹ ; Yingbo Li¹ ; Yufen Zheng ; Laichun Luo ; Qi Sun ; ^{sunqi@bjmu.edu.cn} ; Zemei Ge ; Tieming Cheng ; Runtao Li ; ^{lirt@bjmu.edu.cn}
• 关键词：Multi-target-directed ligands ; Anticancer drugs ; EGFR/HER2 inhibitors ; DNA alkylating agents ; Phosphoramide mustard
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：442-458
• 全文大小：1694 K
• 卷排序：127

文摘

Phosphoramide mustard functionality incorporated into the quinazoline scaffold as EGFR/HER2 inhibitors were proposed. The mechanism studies were supported on DNA damage. Compound 10d is a potential candidate for treatment of lung cancer. MTD study indicated that compound 10d had no obvious acute toxicity.