87033-91-8Relevant academic research and scientific papers
Thioimidazoline based compounds reverse glucocorticoid resistance in human acute lymphoblastic leukemia xenografts
Toscan, Cara E.,Rahimi, Marwa,Bhadbhade, Mohan,Pickford, Russell,McAlpine, Shelli R.,Lock, Richard B.
, p. 6299 - 6312 (2015/06/08)
Glucocorticoids form a critical component of chemotherapy regimens for pediatric acute lymphoblastic leukemia (ALL) and the initial response to glucocorticoid therapy is a major prognostic factor, where resistance is predictive of poor outcome. A high-throughput screen identified four thioimidazoline-containing compounds that reversed dexamethasone resistance in an ALL xenograft derived from a chemoresistant pediatric ALL. The lead compound (1) was synergistic when used in combination with the glucocorticoids, dexamethasone or prednisolone. Synergy was observed in a range of dexamethasone-resistant xenografts representative of B-cell precursor ALL (BCP-ALL) and T-cell ALL. We describe here the synthesis of twenty compounds and biological evaluation of thirty two molecules that explore the structure-activity relationships (SAR) of this novel class of glucocorticoid sensitizing compounds. SAR analysis has identified that the most effective dexamethasone sensitizers contain a thioimidazoline acetamide substructure with a large hydrophobic moiety on the acetamide. This journal is
Synthesis of novel serotonergics and other N-alkylamines using simple reductive amination using catalytic hydrogenation with Pd/C
Karageorge, George N.,Macor, John E.
body text, p. 5117 - 5119 (2011/10/12)
Formation of N-alkylated α-methyltryptamine derivatives (2) was accomplished by simple reductive amination of amine (1) with ketones using catalytic hydrogenation conditions (3 atm H2 and 10% Pd on carbon). This method was also applied to other
Selective synthesis of N-(cyclohexylmethyl)-N-alkylamines from primary amines and pimelaldehyde using tetracarbonylhydridoferrate, HFe(CO)4-, as a reducing reagent
Shim,Kwon,Doh,Kim,Kim
, p. 105 - 106 (2007/10/02)
Treatment of primary amines with pimelaldehyde in the presence of tetracarbonyl-hydridoferrate, HFe(CO)4- at room temperature under atmospheric pressure of CO for 24 hours gave selectively corresponding N-(cyclohexylmethyl)-N-alkylam
