195392-55-3Relevant academic research and scientific papers
The reaction of spiroepoxycyclohexadienones towards cyanide nucleophiles
Córdoba, Rubén,Csák?, Aurelio G.,Plumet, Joaquín,Ortiz, Fernando López,Herrera, Rafael,Jiménez-Vázquez, Hugo A.,Tamariz, Joaquín
, p. 3825 - 3830 (2004)
The reaction of spiroepoxycyclohexadienones 1 with TMSCN in the presence of catalytic amounts of Bu4NCN results in the formation of two diastereomeric cyanohydrins. Alternatively, the reaction of 1 with equimolecular amounts of Bu4NC
Synthesis and biological evaluation of aeroplysinin analogues: a new class of receptor tyrosine kinase inhibitors
Hinterding, Klaus,Knebel, Axel,Herrlich, Peter,Waldmann, Herbert
, p. 1153 - 1162 (2007/10/03)
Receptor tyrosine kinases (RTKs), such as the epidermal growth factor receptor (EGFR) and the platelet-derived growth factor receptor (PDGFR), are critically involved in the transduction of mitogenic signals across the plasma membrane and therefore in the regulation of cell growth and proliferation. Enhanced RTK activity is associated with proliferative diseases such as cancer, psoriasis and atherosclerosis, while decreased function may be associated for instance with diabetes. EGFR and PDGFR are selectively inhibited by analogues of the marine natural product aeroplysinin. The synthetic inhibitors display IC50 values in the low micromolar range and in contrast to the natural product show pronounced inhibitory activity in cultured cells in vivo. The mechanism of inhibition is likely based on a covalent modification of the target enzymes by reaction of epoxy ketone 8 with various nucleophiles. Copyright (C) 1998 Elsevier Science Ltd.
Selective inhibition of receptor tyrosine kinases by synthetic analogues of aeroplysinin
Waldmann,Hinterding,Herrlich,Rahmsdorf,Knebel
, p. 1541 - 1542 (2007/10/03)
IC50 values in the low micromolar range for the inhibition of receptor tyrosine kinases, which are critically involved in the transduction of mitogenic signals and thus in the regulation of cell growth and proliferation, are characteristic of synthetic analogues of marine natural product aeroplysinin 1 such as 2. In addition, they show pronounced inhibitory activity in cultured cells in vivo.
