959237-68-4Relevant articles and documents
Synthesis, Inhibitory Activity, and in Silico Modeling of Selective COX-1 Inhibitors with a Quinazoline Core
Dvorakova, Marcela,Langhansova, Lenka,Temml, Veronika,Pavicic, Antonio,Vanek, Tomas,Landa, Premysl
, p. 610 - 616 (2021/04/07)
Selective cyclooxygenase-1 (COX-1) inhibition has got into the spotlight with the discovery of COX-1 upregulation in various cancers and the cardioprotective role of COX-1 in control of thrombocyte aggregation. Yet, COX-1-selective inhibitors are poorly explored. Thus, three series of quinazoline derivatives were prepared and tested for their potential inhibitory activity toward COX-1 and COX-2. Of the prepared compounds, 11 exhibited interesting COX-1 selectivity, with 8 compounds being totally COX-1-selective. The IC50 value of the best quinazoline inhibitor was 64 nM. The structural features ensuring COX-1 selectivity were elucidated using in silico modeling.
CD73 INHIBITORS
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Paragraph 118, (2020/10/27)
Disclosed are compounds that are inhibitors of CD73 and are useful in treating CD73-associated diseases or conditions, and compositions containing the compounds.
HETEROCYCLIC COMPOUNDS AS PRMT5 INHIBITORS
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, (2019/06/23)
The present disclosure describes novel PRMT5 inhibitors and methods for preparing them. The pharmaceutical compositions comprising such PRMT5 inhibitors and methods of using them for treating cancer, infectious diseases, and other PRMT5 associated disorde