287192-97-6Relevant articles and documents
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)
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.].
Novel RET inhibitors. Pharmaceutical composition and use thereof
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, (2021/11/10)
The invention belongs to the field of medicines, and relates to a novel RET inhibitor, a pharmaceutical composition and application thereof. , The present invention relates to a compound represented by formula (I), a stereoisomer, a tautomer, an oxynitrid
SUBSTITUTED 1, 6-NAPHTHYRIDINE INHIBITORS OF CDK5
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Page/Page column 55; 57-58, (2021/04/10)
Disclosed are compounds having structural formula I, and related salts and pharmaceutical compositions. Also disclosed are therapeutic methods, e.g., of treating diseases and conditions such as kidney disease, kidney failure, kidney stones, or polycystic kidney disease, using the compounds of formula (I), and related salts and pharmaceutical compositions.