A series of 1-acyl-4-phenyl/(acridin-9-yl)thiosemicarbazides 3, including four new compounds, were prepared in order to study substituent effects on cyclization reactions with oxalyl chloride (producing imidazolidine-4,5-diones 4), dimethyl acetylenedicarboxylate (to give thiazolidin-4-ones 7 and 8) and autocondensation under alkaline conditions (to yield 1,2,4-triazoles 9). A positional isomer, 10 of compound 3f was also prepared. Altogether, twenty new compounds characterized and identified by IR, UV, 1H, 13C and 2D NMR and quantum chemical calculations are described. The tautomerism of the products and regioselectivity of the reactions were evaluated. Compounds 3f–h, 3h∙2HCl, 7b,d and 10 were screened for cytotoxic activity against the L1210 leukemia cell line and all compounds, except for 3f, exhibited promising inhibitions of cell growth.
The metal complexes have a significant role in photodynamic therapy (PDT). The most common metals studied for PDT of tumors are transitional metals. In this paper we have studied the copper(II) complexes of N-salicyliden-L-glutamate. The photocytostatic effect was monitored against mouse leukemic cell line L1210. Photocytostatic effect was confirmed for [Cu(N-salicyliden-L-glutamato・2H2O]・isoquinoline (CuCIQ), but it wasn’t observed for the parental molecule [Cu(N-salicyliden-L-glutamato・2H2O]・H2O. CuCIQ had photocytotoxic effect already at 10 μM concentration. Irradiated cells (1050 mJ.cm-2, λ = 365 nm) had half the viability of the cells incubated with CuCIQ in the dark (72 h). Co-incubation of the cells with CuCIQ and ascorbic acid increased this photocytotoxic effect and this effect correlated with the elevated level of lipoperoxidation.
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