1669-85-8Relevant articles and documents
Ru-Catalyzed Switchable N-Hydroxyethylation and N-Acetonylation with Crude Glycerol
Xin, Zhuo,Jia, Le,Huang, Yuxing,Du, Chen-Xia,Li, Yuehui
, p. 2007 - 2011 (2020/03/19)
Highly efficient Ru-catalyzed selective C?C or C?O bond cleavage of polyols (e.g., crude glycerol) for N-hydroxyethylation or N-acetonylation of amines was achieved through the hydrogen-borrowing approach. A variety of amines were transformed to the desired amino alcohols/ketones in moderate-to-excellent yields, opening up new avenues for generation of oxygenated pharmaceuticals and fine chemicals from renewable raw materials. The use of new redox-active catalysts containing bisphosphine/thienylmethylamine ligands allows this hydrogen-borrowing system to be operated selectively under both basic and acidic conditions.
Novel ROS-activated agents utilize a tethered amine to selectively target acute myeloid leukemia
Bell-Horwath, Tiffany R.,Vadukoot, Anish K.,Thowfeik, Fathima Shazna,Li, Guorui,Wunderlich, Mark,Mulloy, James C.,Merino, Edward J.
, p. 2951 - 2954 (2013/06/27)
This study explores the possible use of reactive oxygen-activated DNA modifying agents against acute myeloid leukemia (AML). A key amine on the lead agent was investigated via cytotoxicity assays and was found necessary for potency. The two best compounds were screened via the NCI-60 cell panel. These two compounds had potency between 200 and 800 nM against many of the leukemia cancer cell types. Subsequent experiments explored activity against a transformed AML model that mimics the molecular signatures identified in primary AML patient samples. A lead compound had an IC50 of 760 nM against this AML cell line as well as a therapeutic index of 7.7 ± 3 between the transformed AML model cell line and non-cancerous human CD34+ blood stem/progenitor cells (UCB). The selectivity was much greater than the mainstays of AML treatment: doxorubicin and cytarabine. This manuscript demonstrates that this novel type of agent may be useful against AML.
Synthesis and pharmacological activity of some new pyridazinones
Corsano, S,Strappaghetti, G,Codagnone, A,Scapicchi, R,Marucci, G
, p. 545 - 549 (2007/10/02)
The synthesis of a series of piperazinyl-pyridazinones is reported. The blocking activity of these compounds was determined on the pre- and postsynaptic α-adrenoreceptors of isolated rat vas deferens. For compounds 7, 17 and 18, the hypotensive activity w