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Synthesis and cytotoxicity evaluation of 4-amino-4-dehydroxylarctigenin derivatives in glucose-starved A549 tumor cells

Lei, Min ; Gan, Xianwen ; Zhao, Kun ; Yu, Qiang ; Hu, Lihong

Bioorganic & Medicinal Chemistry Letters, 01 February 2015, Vol.25(3), pp.435-437 [Peer Reviewed Journal]

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  • Title:
    Synthesis and cytotoxicity evaluation of 4-amino-4-dehydroxylarctigenin derivatives in glucose-starved A549 tumor cells
  • Author: Lei, Min ; Gan, Xianwen ; Zhao, Kun ; Yu, Qiang ; Hu, Lihong
  • Description: The natural product arctigenin (ATG) demonstrated preferential cytotoxicity to cancer cells under glucose starvation. A series of 4-amino-4-dehydroxylarctigenin derivatives based on lead compound ATG were designed and synthesized by bioisosteric modifications. Their cytotoxicities were evaluated in glucose-starved A549 tumor cells and the results indicated that the 4-amino-4-dehydroxylarctigenin showed more potent cytotoxicity than arctigenin, and the further substituent group on 4-amino would result in the cytotoxicities decreased significantly. 4-Substituted-arctigenin could selectively target on glucose-starved A549 tumor cells which provide an alternative strategy for anticancer drug development with minimal normal tissue toxicity.
  • Is Part Of: Bioorganic & Medicinal Chemistry Letters, 01 February 2015, Vol.25(3), pp.435-437
  • Identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/j.bmcl.2014.12.061
  • Subjects: Arctigenin (Atg) ; Natural Product ; Glucose Starvation ; 4-Amino-4-Dehydroxylarctigenin ; Bioisosterism ; Medicine ; Chemistry ; Anatomy & Physiology
  • Language: English

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