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Alkyl xanthines underwent
selective homolytic aromatic substitution at C-8 position with alkyl groups of
pentaamminecobalt(III) complex. In this process of synthesis, we used monoalkyl
hydrazines as the radical source in aqueous ammonia solution. Evidence supporting
coordination of the alkyl hydrazine to pentaamminecobalt(III) complex by
radical trapping was in good agreement with literature. The products were
characterized using GC-MS and 1H, 14N and 59Co
A series of 8-substituted alkyl
xanthines were evaluated in vitro to test the cytotoxocity in cells.
For this experiment, we utilized different mammalian cancer cell lines
primarily representing prostrate and lung. One of the compounds synthesized, viz. 8-tertbutyl caffeine showed potent anticancer activity at low concentrations
against DU145 when compared to adriamycin. Further experiments were carried out to check the cell cycle arrest in
the DU145 cells treated with adriamycin, caffeine and 8-tert butyl caffeine. We
observed that there was an arrest in G1 phase of cell cycle at 24 hours while at
48 hours of incubation, the cells
were constantly distributed (59.71% -70.79%). We conclude that the effect of
8-tertbutyl caffeine is relatively comparable to caffeine whereas in adriamycin
treated cells, we observed the cells underwent G2 arrest. We evaluate the
studies on these effects by showing potent analogues which could be used as promising anticancer agents.
suppressor protein 53 (TP53 or simply p53) is a well known protein linked to
apoptosis, cell signalling, cascading and several myriad functions in cells.
Many diseases are linked to p53 though analysis show only 216 interaction
partners. Whether p53 plays an important role in cardiovascular diseases (CVD)
remains uncertain. Through this bioinformatical analysis, we propose that p53
might play a major role in CVD whilst being linked to Hypoxia and Lupus. There
could be evidence by pull down assay studies. Whether its interactants play a
role in CVD remains to be studied using experiments, though the interaction
maps show possible affect on other diseases.