-Lithiation driven one-pot synthesis of quinazolines [2 + 2 + 2] cascade annulation of halofluorobenzenes with nitriles.

A one-pot synthesis of 2,4-disubstituted quinazoline derivatives from halofluorobenzenes with nitriles was reported, sequential nucleophilic addition and SAr reaction. The advantages of the present approach are transition metal free, easy to operate, and all the starting materials are commercially available.

Structures of human phosphofructokinase-1 and atomic basis of cancer-associated mutations.

Phosphofructokinase-1 (PFK1), the 'gatekeeper' of glycolysis, catalyses the committed step of the glycolytic pathway by converting fructose-6-phosphate to fructose-1,6-bisphosphate. Allosteric activation and inhibition of PFK1 by over ten metabolites and in response to hormonal signalling fine-tune glycolytic flux to meet energy requirements. Mutations inhibiting PFK1 activity cause glycogen storage disease type VII, also known as Tarui disease, and mice deficient in muscle PFK1 have decreased fat stores.