Cytotoxic activity of epsilon-aminocaproylamino acids in breast cancer MCF-7 and fibroblast cell lines.

The effect of H-EACA-L-Cys(S-Bzl)-OH, H-EACA-L-Leu-OH, H-EACA-L-Nle-OH and EACA on the viability of MCF-7 and fibroblast cells was examined. The antibacterial activity of these compounds was also tested. H-EACA-L-Leu-OH and H-EACA-L-Nle-OH showed cytotoxic activity against MCF-7 and fibroblast cell lines, particularly in the highest studied 20 mM concentration. None of the examined dipeptides showed antibacterial activity.

Effect of epsilon-aminocaproyl-S-benzyl-L-cysteine on the activity of plasminogen activators.

The effect of epsilon-aminocaproyl-S-benzyl-L-cysteine on the activation of plasminogen by t-PA. streptokinase and urokinase has been examined using fibrinolytic method. The obtained results have been compared with the obtained results for epsilon-aminocaproic acid and trans-4-(aminomethyl)cyclohexanecarboxylic acid. The inhibition of the plasminogen activation determined with the use of epsilon-aminocaproyl-S-benzyl-L-cysteine was weaker than the inhibition determined by using antifibrinolytic aminoacids.

Synthesis and antibacterial activity of DL-threo-1-(1-methylsulfonylpyrrole-3-yl)-2-difluoroacetamidopropane-1,3-diol.

The three-stage synthesis of a pyrrole analogue of chloramphenicol (5) was described. It is inactive.

Pyrrole analogues of chloramphenicol. III. Synthesis and antibacterial activity of DL-threo-1-(1-methylsulfonylpyrrole-3-yl)-2-dichloroacetamidopropane-1,3-diol.

A seven-stage synthesis of a pyrrole analogue of chloramphenicol (9) is described. The compound exhibits a significant antibacterial activity, over the 3% to 50% range of the chloramphenicol activity: over the 6% to 100% range of the thiamphenicol activity and florfenicol.