Add time:07/18/2019         Source:sciencedirect.com

New mono Mannich bases, (2-(4-hydroxy-3-((4-substituephenylpiperazin-1-yl)methyl)benzylidene)-2,3-dihydro-1H-inden-1-one), were prepared to evaluate their cytotoxic/anticancer properties and also their inhibitory effects on human carbonic anhydrase I and II isoenzymes (hCA I and II). Amine part was changed as [N-phenylpiperazine (1), N-benzylpiperazine (2), 1-(2-fluorophenyl)piperazine (3), 1-(4-fluorophenyl)piperazine (4), 1-(2-methoxyphenyl)piperazine (5)]. The structure of the synthesized compounds was characterized 1H-NMR, 13C-NMR and HRMS spectra. Cytotoxicity results of the series pointed out that the compounds 4 had the highest Tumour Selectivity value (TS: 59.4) possibly by inducing necrotic cell death in series. Additionaly, all compunds synthesized showed a good inhibition profile towards hCA I and II isoenzymes with the Ki values between 29.6-58.4 nM and 38.1-69.7 nM, respectively. These values were lower than the reference compound AZA. However, it seems that the compounds 4 and 2 can be considered as lead compounds of CA studies with the lowest Ki values in series for further designes.

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