738577-08-7Relevant articles and documents
TARGETED BIFUNCTIONAL DEGRADERS
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Page/Page column 166; 167, (2021/04/17)
The present invention provides, in one aspect, bifunctional compounds that can be used to promote or enhance degradation of certain circulating proteins. In another aspect, the present invention provides bifunctional compounds that can be used to promote or enhance degradation of certain autoantibodies. In certain embodiments, treatment or management of a disease and/or disorder requires degradation, removal, or reduction in concentration of the circulating protein or the autoantibody in the subject. Thus, in certain embodiments, administration of a compound of the invention to the subject removes or reduces the circulation concentration of the circulating protein or the autoantibody, thus treating, ameliorating, or preventing the disease and/or disorder. In certain embodiments, the circulating protein is TNF.
Design and synthesis of novel triazolo-lapatinib hybrids as inhibitors of breast cancer cells
Shi, YeHui,Zhang, Wei,Li, Lixin,Tong, ZhongSheng,Bai, CuiGai
, p. 2437 - 2445 (2018/11/10)
A series of triazolo-lapatinib hybrids were synthesized via copper (II)-oxide nanoparticle (Cu2O-NP)-catalyzed azide-alkyne cycloaddition. The ability of these compounds to reduce the viability of breast cancer SKBR3 and SUM159 cells and stem cell-like KG-1a leukemia cells was subsequently evaluated. Compared with lapatinib, compounds 6c–f were more potent than lapatinib against the three cell lines. Next, the toxicity of compounds 6c–f was assessed in zebrafish. Compound 6d had comparable toxicity with lapatinib at 200 μM (mortality rate = 10 vs. 10%), and compound 6e had lower toxicity than lapatinib at 200 μM (mortality rate = 0 vs. 10%). Thus, compound 6e is a promising lead compound worthy of further investigation. [Figure not available: see fulltext.].
Discovery of a potent small molecule IL-2 inhibitor through fragment assembly
Braisted, Andrew C.,Oslob, Johan D.,Delano, Warren L.,Hyde, Jennifer,McDowell, Robert S.,Waal, Nathan,Yu, Chul,Arkin, Michelle R.,Raimundo, Brian C.
, p. 3714 - 3715 (2007/10/03)
Using a site-directed fragment discovery method called tethering, we have identified a 60 nM small molecule antagonist of a cytokine/receptor interaction (IL-2/IL2Rα) with cell-based activity. Starting with a low micromolar hit, we employed a combination