Publications by authors named "Mahesh Dighe"
Article Synopsis
- A new series of compounds, including 1,3-diketone and heterocyclic derivatives, were created and tested for their ability to inhibit AhR activity using both zebrafish and mammalian cell models.
- Compounds 1b, 2c, 3b, and 5b demonstrated noticeable AhR antagonist activity, particularly in a transgenic zebrafish model.
- Among these, compounds 3b and 5b stood out with very low inhibition concentrations (3.36 nM and 8.3 nM), and compound 5b also significantly promoted hematopoietic stem cell (HSC) expansion.
Pyruvate dehydrogenase kinase 4 (PDK4) activation is associated with metabolic diseases including hyperglycemia, insulin resistance, allergies, and cancer. Structural modifications of hit anthraquinone led to the identification of a new series of allosteric PDK4 inhibitors. Among this series, compound 8c showed promising in vitro activity with an IC value of 84 nM.
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