653593-69-2Relevant articles and documents
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with in Vivo Efficacy in Multiple Myeloma
Rabal, Obdulia,San José-Enériz, Edurne,Agirre, Xabier,Sánchez-Arias, Juan Antonio,De Miguel, Irene,Ordo?ez, Raquel,Garate, Leire,Miranda, Estíbaliz,Saéz, Elena,Vilas-Zornoza, Amaia,Pineda-Lucena, Antonio,Estella, Ander,Zhang, Feifei,Wu, Wei,Xu, Musheng,Prosper, Felipe,Oyarzabal, Julen
, p. 3392 - 3426 (2021/04/06)
Concomitant inhibition of key epigenetic pathways involved in silencing tumor suppressor genes has been recognized as a promising strategy for cancer therapy. Herein, we report a first-in-class series of quinoline-based analogues that simultaneously inhibit histone deacetylases (from a low nanomolar range) and DNA methyltransferase-1 (from a mid-nanomolar range, IC50 1 log unit), and a suitable pharmacokinetic profile. In vivo, 12a achieved significant antitumor efficacy in a xenograft mouse model of human multiple myeloma.
HETEROCYCLIC COMPOUNDS, MEDICAMENTS CONTAINING SAID COMPOUNDS, USE THEREOF AND PROCESSES FOR THE PREPARATION THEREOF
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Paragraph 0162-0165, (2014/04/03)
The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.