Add time:08/14/2019         Source:sciencedirect.com

Complexes [In(2Ac4Ph)2]NO3·H2O (1), [In(2Ac4mClPh)2]NO3·1.5H2O (2), [In(2Ac4pClPh)2]NO3·2H2O (3) and [In(2Ac4pIPh)2]NO3·H2O (4) were obtained with N(4)-phenyl-2-acetylpyridine thiosemicarbazone (H2Ac4Ph), and its N(4)-meta-chlorophenyl-(H2Ac4mClPh), N(4)-para-chlorophenyl-(H2Ac4pClPh) and N(4)-para-iodophenyl-(H2Ac4pIPh) derivatives. The crystal structures of [In(2Ac4Ph)2]NO3·MeOH (1a), [In(2Ac4mClPh)2]NO3·EtOH·H2O (2a) and [In(2Ac4pClPh)2]·NO3 (3a) were determined. The cytotoxic effects of the thiosemicarbazone ligands and of complexes (1–4) were evaluated against HL-60, Jurkat and THP-1 leukemia cells and against MCF-7, MDA-MB-231 and HCT-116 solid tumor cells, as well as against mammalian healthy Vero cells. Upon coordination to indium(III) cytotoxicity increased in several cases. In addition, complex (1) was active in sub-micromolar doses against all tested cell lineages, with selectivity indexes (SI = IC50 Vero/IC50 tumor cell) ranging from 3 (against THP-1 cells) to 144 (against HCT-116 cells).

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