The regioselective synthesis of spirooxindolo pyrrolidines and pyrrolizidines via three-component reactions of acrylamides and aroylacrylic acids with isatins and α-amino acids

• Tatyana L. Pavlovskaya,
• Fedor G. Yaremenko,
• Victoria V. Lipson,
• Svetlana V. Shishkina,
• Oleg V. Shishkin,
• Vladimir I. Musatov and
• Alexander S. Karpenko

Beilstein J. Org. Chem. 2014, 10, 117–126, doi:10.3762/bjoc.10.8

• commutatа [4], mitraphylline from Uncaria tomentosa [5] and spirotryprostatines A and B from the secondary metabolites of Aspergillus fumigatus [6][7][8]. In particular, oxindole derivatives are well known as powerful anti-tumor agents due to their kinase inhibitory properties, especially as tyrosine kinase

Dimerization of a cell-penetrating peptide leads to enhanced cellular uptake and drug delivery

• Jan Hoyer,
• Ulrich Schatzschneider,
• Michaela Schulz-Siegmund and
• Ines Neundorf

Beilstein J. Org. Chem. 2012, 8, 1788–1797, doi:10.3762/bjoc.8.204

• a cell-penetrating peptide. Keywords: anti-tumor agents; cell-penetrating peptides; drug delivery; internalization studies; organometallic complexes; peptides; Introduction A substantial problem concerning promising drug candidates is often their incapacity to reach their full therapeutic

• at different concentrations after 1 h incubation. Experiments were conducted in triplicate with n = 2. Error bars represent the standard deviation. Synthesis of (sC18)2 bioconjugates (a) and chemical structures of the coupled anti-tumor agents (b). Mtt: 4-methyltrityl chloride; Dde: 1-(4,4-dimethyl