1308685-75-7Relevant academic research and scientific papers
Synthesis and activity of n-sulfonylamides of tripeptides as potential urokinase inhibitors
Markowska, Agnieszka,Bruzgo, Irena,Miltyk, Wojciech,Midura-Nowaczek, Krystyna
experimental part, p. 1300 - 1304 (2011/12/16)
Twelve peptides of the general X-SO2-D-Ser-Ala-Arg-OH formula (where X = methyl, phenyl,α-tolyl, p-tolyl,4-methylbenzyl,1-naphtyl,2-naphtyl,4-chlorophenyl,4-bromophenyl,2-mesityl,2,4,6-triisopropylphenyl,4-acet-amidophenyl) were obtained and tested for their effect on the amidolytic activities of urokinase, thrombin, trypsin, plas- min, t-PA and kallikrein. 2,4,6-triisopropylphenyl-SO2-D-Ser-Ala-Arg-OH was the most selective inhibitor of urokinase and -tolyl-SO2-D-Ser-Ala-Arg-OH was the most active inhibitor of uPA with Ki value 24 μM. The compounds were tested for their in vitro antitumour activity in the following human breast cancer cells: standard MCF-7 and estrogen- independent MDA-MB-231. Four of the synthesized peptides showed cytotoxic effects against MDA-MB-231 cell lines in the range from 2.9 to 8.5 μM. The examined compound did not influence to MCF 7 cancer cells. The synthesized peptides were nontoxic to pig's erythrocytes.
