Chemistry, like all the natural sciences, Category: pyridazines, begins with the direct observation of nature¡ª in this case, of matter.920-66-1, Name is 1,1,1,3,3,3-Hexafluoropropan-2-ol, SMILES is OC(C(F)(F)F)C(F)(F)F, belongs to pyridazines compound. In a document, author is Martinez-Gonzalez, Sonia, introduce the new discover.
Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors
PIM kinase family (PIM-1, PIM-2 and PIM-3) is an appealing target for the discovery and development of selective inhibitors, useful in various disease conditions in which these proteins are highly expressed, such as cancer. The significant effort put, in the recent years, towards the development of small molecules exhibiting inhibitory activity against this protein family has ended up with several molecules entering clinical trials. As part of our ongoing exploration for potential drug candidates that exhibit affinity towards this protein family, we have generated a novel chemical series of triazolo[4,3-b]pyridazine based tricycles by applying a scaffold hopping strategy over our previously reported potent pan-PIM inhibitor ETP-47453 (compound 2). The structure-activity relationship studies presented herein demonstrate a rather selective PIM-1 /PIM-3 biochemical profile for this novel series of tricycles, although pan-PIM and PIM-1 inhibitors have also been identified. Selected examples show significant inhibition of the phosphorylation of BAD protein in a cell-based assay. Moreover, optimized and highly selective compounds, such as 42, did not show significant hERG inhibition at 20 mu M concentration, and proved its antiproliferative activity and utility in combination with particular antitumoral agents in several tumor cell lines. (C) 2019 Elsevier Masson SAS. All rights reserved.
Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions. you can also check out more blogs about 920-66-1. Category: pyridazines.
Reference:
Pyridazine – Wikipedia,
,Pyridazine | C4H4N2 – PubChem