title: Investigation on the pharmacological profile of 2,6-diacetylpyridine bis(benzoylhydrazone) derivatives and their antimony(III) and bismuth(III) complexes.
abstract: Complexes [Sb(HAcPh)Cl(2)] (1), [Sb(HAcpClPh)Cl(2)] (2), [Sb(HAcpNO(2)Ph)Cl(2)] (3) and [Bi(HAcPh)Cl(2)] (4), [Bi(HAcpClPh)Cl(2)] (5), [Bi(HAcpNO(2)Ph)Cl(2)] (6) were obtained with 2,6-diacetylpyridine bis(benzoylhydrazone) (H(2)AcPh), 2,6-diacetylpyridine bis(para-chlorobenzoylhydrazone) (H(2)AcpClPh), and 2,6-diacetylpyridine bis(para-nitrobenzoylhydrazone) (H(2)AcpNO(2)Ph). 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.
authors.affiliation: Departamento de Química, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, MG, Brazil.
authors.forename: Karina S O
authors.initials: KS
authors.lastname: Ferraz
authors.forename: Nayane F
authors.initials: NF
authors.lastname: Silva
authors.forename: Jeferson G
authors.initials: JG
authors.lastname: da Silva
authors.forename: Luana F
authors.initials: LF
authors.lastname: de Miranda
authors.forename: Carla F D
authors.initials: CF
authors.lastname: Romeiro
authors.forename: Elaine M
authors.initials: EM
authors.lastname: Souza-Fagundes
authors.forename: Isolda C
authors.initials: IC
authors.lastname: Mendes
authors.forename: Heloisa
authors.initials: H
authors.lastname: Beraldo
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000965:Antimony / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D001729:Bismuth / Q000737:chemistry*; D002176:Candida albicans / Q000187:drug effects; D045744:Cell Line, Tumor; D006801:Humans; D008826:Microbial Sensitivity Tests; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011725:Pyridines / Q000737:chemistry*
chemical_list: D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D011725:Pyridines; D000965:Antimony; C023666:pyridine; D001729:Bismuth