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Structure– activity relationship between the nitrogen mustards of isatin and their effects on HeLa cells

Congeneric series of isatin N– Mannich bases with nitrogen mustard moiety was synthesized and tested for biological activity. Acute effects of the studied Mannich bases on cultured HeLa cells were killing and depression of 3H– thymidine incorporation. Among these two cellular responses 3H– thymidine incorporation experiment was found to be more sensitive. Mitodepressive activity of isatin nitrogen mustards 1– 10 was determined in a phyto test on Lepidium sativum L. Comparing results from all studies it was found that 5-nitro substituted Mannich bases are less biologically active than the analogues of 5-non-substituted parent molecule. Furthermore, results from HeLa cell culture studies show a parabolic dependence of the biological activity on the lipophylic properties. The ideal lipofilicity (log P0) for the maximum activity of the inhibition of HeLa cells is not significantly different from that of inhibiting 3H– thymidine incorporation unto DNA, considering the overlap of the 95% confidence limits.

nitrogen mustards of isatine; SAR; HeLa cells

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