16874-54-7Relevant academic research and scientific papers
Parallel synthesis of bis-oxazole peptidomimetics
Murru, Siva,Dooley, Colette T.,Nefzi, Adel
, p. 7062 - 7064 (2013)
The parallel synthesis of bis-oxazole peptidomimetics starting from Boc-aminoacids and Serine-methyl ester is described. This work presents the synthesis of oxazole aminoacid building blocks in solution phase and their utilization for the solid phase pept
Synthesis and anti-cancer activity of naturally occurring 2,5-diketopiperazines
Mollica, Adriano,Costante, Roberto,Fiorito, Serena,Genovese, Salvatore,Stefanucci, Azzurra,Mathieu, Veronique,Kiss, Robert,Epifano, Francesco
, p. 91 - 97 (2014/08/18)
Three naturally occurring oxyprenylated diketopiperazines were synthesized and preliminarily tested as growth inhibitory agents in vitro against various cancer cell lines. The compounds were tested on six human cancer cell lines with different sensitivity to proapoptotic stimuli using the MTT colorimetric assay. The data revealed that of the chemicals under study only deoxymicelianamide (11) displayed the highest activity, recording mean IC50 growth inhibitory values ranging from 2 to 23 μM. A comparative study with the non-geranylated saturated derivative of (11) revealed the importance of the presence of the geranyloxy side chain and the exocyclic 2,5-DPK double bond moiety for the observed activity.
Protection of Hydroxy Groups by Silylation: Use in Peptide Synthesis and as Lipophilicity Modifiers for Peptides
Davies, John S.,Higginbotham, Clement L.,Tremeer, E. John,Brown, Charles,Treadgold, Richard C.
, p. 3043 - 3048 (2007/10/02)
A survey of a series of organosilyl derivatives of serine and tyrosine has shown that they have a satisfactory stability profile for use in peptide synthesis.Only when alkaline conditions were used did side-reactions appear.A range of stability profiles have been determined from a study of organosilyl derivatised dipetides under different conditions, giving t1/2 values for hydrolysis ranging from 41 to 465 min in acid conditions, yet giving long-term stability at pH-values near to neutrality.
