Reference of 65-71-4, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, 65-71-4, Name is 5-Methylpyrimidine-2,4(1H,3H)-dione, SMILES is O=C1NC(C(C)=CN1)=O, belongs to pyrimidines compound. In a article, author is Wang, Shuai, introduce new discover of the category.
Structure-Based Design, Synthesis, and Biological Evaluation of New Triazolo[1,5-a]Pyrimidine Derivatives as Highly Potent and Orally Active ABCB1 Modulators
ABCB1 is a promising therapeutic target for overcoming multidrug resistance (MDR). In this work, we reported the structure-based design of triazolo[1,5-a]pyrimidines as new ABCB1 modulators, of which WS-691 significantly increased sensitization of ABCB1-overexpressed SW620/Ad300 cells to paclitaxel (PTX) (IC50 = 22.02 nM). Mechanistic studies indicated that WS-691 significantly increased the intracellular concentration of PTX and [H-3]-PTX while decreasing the efflux of [H-3]-PTX in SW620/Ad300 cells by inhibiting the efflux function of ABCB1. The cellular thermal shift assay suggested that WS-691 could stabilize ABCB1 by directly binding to ABCB1. WS-691 could stimulate the activity of ABCB1 ATPase but had almost no inhibitory activity against CYP3A4. Importantly, WS-691 increased the sensitivity of SW620/Ad300 cells to PTX in vivo without observed toxicity. Collectively, WS-691 is a highly potent and orally active ABCB1 modulator capable of overcoming MDR. The triazolo[1,5-a]dpyrimidine may be a promising scaffold for developing more potent ABCB1 modulators.
Reference of 65-71-4, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 65-71-4 is helpful to your research.
Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia