86905-46-6Relevant academic research and scientific papers
Bridgehead Modifications of Englerin A Reduce TRPC4 Activity and Intravenous Toxicity but not Cell Growth Inhibition
Wu, Zhenhua,Suppo, Jean-Simon,Tumova, Sarka,Strope, Jonathan,Bravo, Fernando,Moy, Melody,Weinstein, Ethan S.,Peer, Cody J.,Figg, William D.,Chain, William J.,Echavarren, Antonio M.,Beech, David J.,Beutler, John A.
, p. 1711 - 1716 (2020)
Modifications at the bridgehead position of englerin A were made to explore the effects of variation at this site on the molecule for biological activity, as judged by the NCI 60 screen, in which englerin A is highly potent and selective for renal cancer cells. Replacement of the isopropyl group by other, larger substituents yielded compounds which displayed excellent selectivity and potency comparable to the natural product. Selected compounds were also evaluated for their effect on the ion channel TRPC4 as well as for intravenous toxicity in mice, and these had lower potency in both assays compared to englerin A.
ETHYL 5-SUBSTITUTED-3-ISOXAZOLECARBOXYLATES AS STARTING MATERIALS FOR A CONVENIENT ROUTE TO 3(2H)FURANONES AND 3(2H)IMINOFURANES.
Baraldi, Pier Giovanni,Barco, Achille,Benetti, Simonetta,Manfredini, Stefano,Pollini, Gian Piero,Simoni, Daniele
, p. 4313 - 4316 (2007/10/02)
Cyclodehydration of γ-hydroxy-β-enaminoketones derived from 5-substituted-3-isoxazolemethanols leads to 3(2H)furanones or 3(2H)iminofuranes depending on the substitution pattern and on the reaction conditions.
REDUCTION OF Δ2-ISOXAZOLINES-2. A FACILE SYNTHESIS OF 3(2H)-FURANONES.
Curran, Dennis P.,Singleton, David H.
, p. 2079 - 2082 (2007/10/02)
A simple synthesis of the 3(2H)-furanone ring system is described.
SILYL NITRONATES IN ORGANIC SYNTHESIS. SYNTHESIS OF 3(2H)-FURANONES
Andersen, Soeren H.,Sharma, K. K.,Torssell, Kurt, B. G.
, p. 2241 - 2246 (2007/10/02)
A synthesis of 3(2H)-furanones, a structural element of several natural products, has been developed in which silyl nitronates or nitrile oxides are condensed with vinyl ketones to form 5-acyl-2-isoxazolines which are reduced with titanous ions or catalytically to 1,4-diketo-2-ols and cyclized with sodium acetate in acetic acid.
