Investigation on the pharmacological profile of 2,6-diacetylpyridine bis(benzoylhydrazone) derivatives and their antimony(III) and bismuth(III) complexes

摘要

Complexes [Sb(HAcPh)Cl 2] (1), [Sb(HAcpClPh)Cl 2] (2), [Sb(HAcpNO 2Ph)Cl 2] (3) and [Bi(HAcPh)Cl 2] (4), [Bi(HAcpClPh)Cl 2] (5), [Bi(HAcpNO 2Ph)Cl 2] (6) were obtained with 2,6-diacetylpyridine bis(benzoylhydrazone) (H 2AcPh), 2,6-diacetylpyridine bis(para-chlorobenzoylhydrazone) (H 2AcpClPh), and 2,6-diacetylpyridine bis(para-nitrobenzoylhydrazone) (H 2AcpNO 2Ph). The bis(benzoylhydrazones) were inactive as antimicrobial agents against gram-positive and gram-negative bacteria and against Candida albicans but upon coordination to antimony(III) and bismuth(III) antimicrobial activity was demonstrated. The studied compounds were tested for their cytotoxic activities against Jurkat and HL60 (leukemia), MCF-7 (breast tumor), HCT-116 (colorectal carcinoma) and peripheral blood mononuclear (PBMC) cells. All bis(benzoylhydrazones) proved to be poorly cytotoxic. Upon coordination of the bis(benzoylhydrazones) to antimony(III) and bismuth(III) cytotoxicity significantly improved. Complex (5) presented high therapeutic indexes (TI = 11-508) against all cell lineages.