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: shidayong@qdio.ac.cn.

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.

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