2. Academic Validation
  3. Synthesis and cytotoxicity evaluation of 4-amino-4-dehydroxylarctigenin derivatives in glucose-starved A549 tumor cells

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

  • Bioorg Med Chem Lett. 2015 Feb 1;25(3):435-7. doi: 10.1016/j.bmcl.2014.12.061.
Min Lei 1,  Xianwen Gan 1,  Kun Zhao 1,  Qiang Yu 1,  Lihong Hu 2
Affiliations

Affiliations

  • 1 Shanghai Research Center for the Modernization of Traditional Chinese Medicine, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China.
  • 2 Shanghai Research Center for the Modernization of Traditional Chinese Medicine, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China. Electronic address: lhhu@simm.ac.cn.
PMID: 25571795 DOI: 10.1016/j.bmcl.2014.12.061
Abstract

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.

Keywords

4-Amino-4-dehydroxylarctigenin; Arctigenin (ATG); Bioisosterism; Glucose starvation; Natural product.

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