Aerobic glycolysis, originally identified by Warburg as a hallmark of cancer, has recently been implicated in immune cell activation and growth. Glucose, the starting material for glycolysis, is transported through the cellular membrane by a family of glucose transporters (GLUTs). Therefore, targeting glucose transporters to regulate aerobic glycolysis is an attractive approach to identify potential therapeutic agents for cancers and autoimmune diseases. Herein, we describe the discovery and optimization of a class of potent, orally bioavailable inhibitors of glucose transporters, targeting both GLUT1 and GLUT3.

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A practical method for the formation of thiophosphonates bearing functionalized monocyclic, fused bicyclic and spirocyclic residues is presented. The procedure requires the easily available terminal alkynes as starting materials as well as commercially and readily available reagents such as diethyl thiophosphite. The experimental procedure consists of a one-pot process without any slow addition of one of the reagents.

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Monocyclic, bicyclic, and spirocyclic 5-membered ring products are available. -(LAMARQUE, C.; BEAUFILS, F.; DENES, F.; SCHENK, K.; RENAUD*, P.; Adv. Synth. Catal. 353 (2011) 8, 1353-1358, http://dx.doi.org/10.1002/adsc.201000852 ; Dep. Chem. Biochem., Univ. Bern, CH-3012 Bern, Switz.; Eng.) -Jannicke 40-177