Bijian, Krikor published the artcileNovel Aurora A and Protein Kinase C (¦Á, ¦Â1, ¦Â2, and ¦È) Multitarget Inhibitors: Impact of Selenium Atoms on the Potency and Selectivity, Quality Control of 119-80-2, the publication is Journal of Medicinal Chemistry (2022), 65(4), 3134-3150, database is CAplus and MEDLINE.
Aurora kinases and protein kinase C (PKC) have been shown to be involved in different aspects of cancer progression. To date, no dual Aurora/PKC inhibitor with clin. efficacy and low toxicity is available. Here, we report the identification of compound 2e as a potent small mol. capable of selectively inhibiting Aurora A kinase and PKC isoforms ¦Á, ¦Â1, ¦Â2 and ¦È. Compound 2e demonstrated significant inhibition of the colony forming ability of metastatic breast cancer cells in vitro and metastasis development in vivo. In vitro kinase screening and mol. modeling studies revealed the critical role of the selenium-containing side chains within 2e, where selenium atoms were shown to significantly improve its selectivity and potency by forming addnl. interactions and modulating the protein dynamics. In comparison to other H-bonding heteroatoms such as sulfur, our studies suggested that these selenium atoms also confer more favorable PK properties.
Journal of Medicinal Chemistry published new progress about 119-80-2. 119-80-2 belongs to catalysis-chemistry, auxiliary class sulfides,Carboxylic acid,Benzene, name is 2,2′-Dithiodibenzoic acid, and the molecular formula is C14H10O4S2, Quality Control of 119-80-2.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia