660852-86-8Relevant articles and documents
ISOINDOLINE COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASE
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, (2015/09/23)
Isoindoline sigma-2 receptor antagonist compounds, pharmaceutical compositions comprising such compounds, and methods for inhibiting Abeta- associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology are provided.
NOVEL PROCESS FOR THE PREPARATION OF (R)-N-BENZYL-2-ACETAMIDO-3-METHOXYPROPIONAMIDE
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Paragraph 0043, (2014/11/11)
The invention is a novel process for the preparation of lacosamide by employing novel intermediates of formula III and IV:
Synthesis of a novel series of 2,3,4-trisubstituted oxazolidines designed by isosteric replacement or rigidification of the structure and cytotoxic evaluation
Andrade, Saulo F.,Teixeira, Claudia S.,Ramos, Jonas P.,Lopes, Marcela S.,Pdua, Rodrigo M.,Oliveira, Mnica C.,Souza-Fagundes, Elaine M.,Alves, Ricardo J.
, p. 1693 - 1699 (2014/12/11)
We have previously reported on a study of the structure-activity relationship in a series of 2,3,4-substituted oxazolidines recently discovered by our group varying the substituent at the ring or stereochemistry of the oxazolidine ring. We discovered the cytotoxic and pro-apoptotic potential of compounds 1 and 2 with good selectivity against cancer cell lines. In the present study we describe the synthesis and cytotoxic evaluation against cancer cell lines (HL60, JURKAT, MDA-MB-231 and LNCaP) of a series of oxazolidines designed by isosteric replacement or rigidification of the oxymethylene spacer of compounds 1 and 2. Alkenes 3 and 4 retained the activity against MDA-MB-231 cells and they were more active on HL60, JURKAT and LNCaP cells. Considering LNCaP cells, E-isomer 4 was at least 7 times and about 3 times more potent than lead 1 and Z-isomer 3, respectively. Compound 4 exerted significant activity against LNCaP with IC50 in the low micromolar range (11 μM) without affecting VERO cells and PBMC proliferation (IC50 > 100 μM) indicating its low toxicity to normal cells.
NMR characterization and conformational analysis of a potent papain-family cathepsin L-like cysteine protease inhibitor with different behaviour in polar and apolar media
Rotondo, Archimede,Ettari, Roberta,Zappalà, Maria,De Micheli, Carlo,Rotondo, Enrico
, p. 337 - 343 (2015/01/16)
We recently reported the synthesis, of a potent papain-family cathepsin L-like cysteine protease inhibitor, as new lead compound for the development of new drugs that can be used as antiprotozoal agents. The investigation of its conformational profile is
Effects on polo-like kinase 1 polo-box domain binding affinities of peptides incurred by structural variation at the phosphoamino acid position
Qian, Wenjian,Park, Jung-Eun,Liu, Fa,Lee, Kyung S.,Burke Jr., Terrence R.
, p. 3996 - 4003 (2013/07/27)
Protein-protein interactions (PPIs) mediated by the polo-box domain (PBD) of polo-like kinase 1 (Plk1) serve important roles in cell proliferation. Critical elements in the high affinity recognition of peptides and proteins by PBD are derived from pThr/pS
Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors
Ettari, Roberta,Nizi, Emanuela,Di Francesco, Maria Emilia,Dude, Marie-Adrienne,Pradel, Gabriele,Vi?ík, Radim,Schirmeister, Tanja,Micale, Nicola,Grasso, Silvana,Zappalà, Maria
, p. 988 - 996 (2008/09/19)
This paper describes the synthesis of a new class of peptidomimetic cysteine protease inhibitors based on a 1,4-benzodiazepine scaffold and on an electrophilic vinyl sulfone moiety. The former was introduced internally to a peptide sequence that mimics th
Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents
Micale, Nicola,Kozikowski, Alan P.,Ettari, Roberta,Grasso, Silvana,Zappalà, Maria,Jeong, Jong-Jin,Kumar, Ajay,Hanspal, Manjit,Chishti, Athar H.
, p. 3064 - 3067 (2007/10/03)
The synthesis of a new class of peptidomimetics 1a-j, based on a 1,4-benzodiazepine scaffold and on a C-terminal aspartyl aldehyde building block, is described. Compounds 1a-j provided significant inhibitory activity against falcipains 2A and 2B (FP-2A an
Synthesis of C-glycosyl amino acids: Scope and limitations of the tandem Tebbe/Claisen approach
Chambers, David J.,Evans, Graham R.,Fairbanks, Antony J.
, p. 45 - 55 (2007/10/03)
Amino acids may be used as coupling partners for esterification with 3-hydroxy glycals as substrates for the tandem Tebbe/Claisen approach to the synthesis of C-glycosyl amino acids. Whilst esters of substituted α-amino acids do not successfully undergo T
Derivatives of glycinergic r(+)-2-amino-3-hydroxypropanoic acid
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Page/Page column 5, (2008/06/13)
The use of R(+)-2-amino-3-hydroxypropanoic acid derivatives, nitrogen substituted by a (C1-C6)alkyl, (C3-C6)alkenyl, 3-oxo(C5-C6)alkyl, 3-oxo(C4-C6)alken-2-yl, phenyl(