Herein, triphenylphosphonium cation moieties were incorporated into a
dichloroacetophenone derivative, leading to the discovery of novel mitochondria-targeted …

Pyruvate dehydrogenase kinases (PDKs) are overexpressed in most cancer cells and are
responsible for aberrant glucose metabolism. We previously described bis (4-morpholinyl …

Dichloroacetophenone is a pyruvate dehydrogenase kinase 1 (PDK1) inhibitor with
suboptimal kinase selectivity. Herein, we report the synthesis and biological evaluation of a …

Warburg effect, a preference of aerobic glycolysis for energy production even in the
presence of adequate oxygen, is one of the most prominent distinctions of cancer cells from …

Metabolism is reprogrammed in a variety of cancer cells to ensure their rapid proliferation.
Cancer cells prefer to utilize glycolysis to produce energy as well as to provide large …

Current drug development in oncology is non-selective as it typically focuses on pathways
essential for the survival of all dividing cells. The unique metabolic profile of cancer, which is …

Targeting pyruvate dehydrogenase kinases (PDKs) reverses the Warburg effect, which
could be a potential therapeutic target for anti-cancer drug discovery. In this paper, we …

Pyruvate dehydrogenase kinases (PDKs) are promising therapeutic targets that have
received increasing attentions in cancer metabolism. In this paper, we report the synthesis …

Targeting pyruvate dehydrogenase kinase 1 (PDK1) has been suggested as a potential
anticancer strategy. 2, 2-dichloroacetophenone (DAP) is a PDK1 inhibitor exhibiting weak …

In many types of cancers, pyruvate dehydrogenase kinase (PDK) is abnormally
overexpressed and has become a promising target for cancer therapy. However, few highly …