Lien, Vegard Torp; Kristiansen, Margrethe Konstanse; Pettersen, Solveig; Haugen, Mads Haugland; Olberg, Dag Erlend; Waaler, Jo; Klaveness, Jo published an article in 2019, the title of the article was Towards dual inhibitors of the MET kinase and WNT signaling pathway; design, synthesis and biological evaluation.Safety of 2-(2-Bromoethyl)isoindoline-1,3-dione And the article contains the following content:
Both the kinase MET and the WNT signaling pathway are attractive targets in cancer therapy, and synergistic effects have previously been observed in animal models upon simultaneous inhibition. A strategy towards a designed multiple ligand of MET and WNT signaling is pursued based on the two hetero biaryl systems present in both the MET inhibitor tepotinib and WNT signaling inhibitor TC-E 5001. Initial screening was conducted to find the most suitable ring systems for further optimization, whereas a second screen explored modifications towards pyridazinones and triazolo pyridazines. Up to 54% reduction of WNT signaling activity at 10 microM concentration was achieved, however, only low affinities towards MET were observed Overall, the thiophene substituted pyridazinone 40 was the best dual MET and WNT signaling inhibitor, with a 17% and 19% reduction of activity, resp. Although further optimizations are needed to achieve more potent dual inhibitors, the strategy presented herein can be valuable towards the development of a dual inhibitor of MET and WNT signaling. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Safety of 2-(2-Bromoethyl)isoindoline-1,3-dione
The Article related to met kinase wnt inhibitor anticancer agent signaling, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Safety of 2-(2-Bromoethyl)isoindoline-1,3-dione
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary