Preparation, spectral properties and biological activities of 5-bromo-6-methyl-2'-deoxyuridine and 5-iodo-6-methyl-2'-deoxyuridine

1980 ◽  
Vol 45 (8) ◽  
pp. 2364-2370 ◽  
Author(s):  
Antonín Holý ◽  
Erik De Clercq

Reaction of 3',5'-di-O-benzoyl-6-methyl-2'-deoxyuridine (IIa) with elementary bromine or iodine afforded 5-halogeno derivatives IIc and IId which on methanolysis gave 5-bromo-6-methyl-2'-deoxyurine (Ic) and 5-iodo-6-methyl-2'-deoxyurine (Id), respectively. The CD spectra of Ic, Id and 6-methyl-2'-deoxyuridine (Ia) are compared and discussed with regard to determination of the nucleoside conformation. Unlike 5-bromo- and 5-iodo-2'-deoxyuridine, the 6-methyl derivatives Ic and Id exhibit neither antibacterial nor antiviral activity. Nor do they exert any antimetabolic effect on the de novo DNA synthesis in primary rabbit kidney cells.

1995 ◽  
Vol 50 (1-2) ◽  
pp. 93-97 ◽  
Author(s):  
Tetsuya Matsuno

Abstract A physiologically active substance has been isolated from Brazilian propolis and charac­terized as a new clerodane diterpenoid, as indicated by human hepatocellular carcinoma HuH 13 cell cytotoxicity assays. This compound inhibited growth of the hepatoma cells at a concentration around 10 μg/ml and arrested the tumor cells at S phase as revealed by flow cytometry. At higher concentrations it exerted lethal damage. The compound showed cyto­toxicity on human lung carcinoma HLC-2, HeLa, KB and rat W3Y cells, whereas human diploid foreskin and primary rabbit kidney cells were less affected.


1979 ◽  
Author(s):  
M. Kopeć ◽  
W. Rosazkowski ◽  
S. Szmigielski ◽  
B. Gerdin ◽  
T. Saldeen

Dialysable peptides of mw 2200 to 3500 D(LMW-FDP) were isolated from products of exhaustive proteolysis of fibrinogen by plasmin. LMW-FDP inhibited in a dose dependent manner incorporation of 3H-thymidme into cultures of human blood lymphocytes simulated with PHA, concanavalin A or bacterial lipopolisaccharide. These effects were inversely related to stimulation indices. Phagocytosis of 3H-thymidine labelled Staphylococcus aureus by mouse peritoneal macrophages was also inhibited by LMW-FDP. These peptides induced a cytotoxic effect on continuous line of rabbit kidney cells in cultures as manifested by inhibition of 86Rb and 3H-incorporation as well as by releese of 86Rb and 61Cr from prelabelled cells. Eight fractions obtained by molecular sieving of LMW - FDP on Bio-Gel P-6 columns were found to differ pronouncedly in biological activities.


1980 ◽  
Vol 35 (9-10) ◽  
pp. 747-749
Author(s):  
E. Jürgen Zöllner ◽  
Rudolf K. Zahn ◽  
Dietrich Falke

Abstract In primary rabbit kidney cells infected with herpes simplex virus four different neutral deoxyribonuclease activities can be detected by means of the deoxyribonuclease assay in DNA-containing polyacrylamide gels following their separation by discelectrophoresis. The method is suitable to follow independently the change in each activity of the different enzymes using only about 5 × 105 cells for each assay during the time-course of infection. Under these conditions one enzyme activity is constant, two disappear while the activity of a fourth one present only in infected cells, increases.


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