Design of antitumor agents containing carbohydrate based on GLUT1, and evaluation of antiproliferative activity

  • Bioorg Med Chem Lett. 2017 Jun 1;27(11):2488-2492. doi: 10.1016/j.bmcl.2017.03.094.
Renshuai Zhang  1 ,  Lairong Song  2 ,  Bo Jiang  1 ,  Lijun Wang  1 ,  Ning Wu  1 ,  Shuju Guo  1 ,  Dayong Shi  3
Affiliations
  • 1. Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences, Qingdao, China; Laboratory for Marine Drugs and Bioproducts, Qingdao National Laboratory for Marine Science and Technology, Qingdao, China.
  • 2. Department of Neurosurgery, The Affiliated Hospital of Qingdao University, Qingdao, China.
  • 3. Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences, Qingdao, China; Laboratory for Marine Drugs and Bioproducts, Qingdao National Laboratory for Marine Science and Technology, Qingdao, China; University of Chinese Academy of Sciences, Beijing, China. Electronic address: [email protected].
PMID: 28462838 DOI: 10.1016/j.bmcl.2017.03.094
Abstract

A series of novel carbohydrate-modified antitumor compounds were designed based on glucose transporter 1 (GLUT1), and evaluated for their Anticancer activities against four Cancer cell lines. The ribose derivatives (compound 9 and 10) exhibited modest inhibitory activity. The compound 9 significantly inhibited the migration of A549 cell and induced A549 cell Apoptosis in a concentration-dependent manner. Moreover, compound 9 blocked A549 cells at the G0/G1 phase. The cellular uptake studies suggested that ribose-modified compound 9 could be taken through GLUT1 in A549 cell line.

Keywords
Anticancer; Cell uptake; Drug design; GLUT1; Saccharide.