Cancer cells metabolism is different from that of normal cells and its progression involves an uncontrolled capacity for cell proliferation supplied by increased glucose uptake via membrane-spanning proteins called glucose transporters (GLUTs). Since it is well recognized that glucose deprivation results in cancer cell death, targeting glucose uptake in cancer cells becomes a promising strategy to combat cancer. Considering such a perspective, the development of potential anticancer agents has become the focus of the current study. We followed our goal through the design and synthesis of novel molecular frameworks investigating the impact of conformational restriction as well as functional group interconversions on inhibitory activities shown by DRB-18 as our current lead GLUT inhibitor. Finally, the structure-activity relationships of these compounds as both inhibitors of glucose transport and cancer cell proliferation were measured via corresponding assays in human cancer cell lines. These set of compounds have been proposed to pave the way toward introducing GLUT inhibitors with improved physiological stability and anticancer efficacy.

Development of small-molecule glucose uptake transporter inhibitors as potential anticancer agents

Where thousands of chemistry professionals meet to share ideas and advance scientific and technical knowledge. Spring 2023 abstracts, posters, and presentations will launch at the end of March.

ACS Spring 2023

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.