ABSTRACT
Aliphatic and aromatic ferrocenylthiosemicarbazones were synthesized. The characterization of the new ferrocenylthiosemicarbazones was done by IR, (1)H-NMR and (13)C-NMR spectroscopy, elemental analysis and X-ray diffraction studies. The biological activity of the obtained compounds was assessed in terms of anticancer activity. Their activity against U251 (human glyoblastoma), PC-3 (human prostatic adenocarcinoma), K562 (human chronic myelogenous leukemia), HCT-15 (human colorectal adenocarcinoma), MCF-7 (human mammary adenocarcinoma) and SKLU-1 (human lung adenocarcinoma) cell lines was studied and compared with cisplatin. All tested compounds showed good activity and the aryl-chloro substituted ferrocenylthiosemicarbazones showed the best anticancer activity.
Subject(s)
Antineoplastic Agents/pharmacology , Coordination Complexes/pharmacology , Ferrous Compounds/pharmacology , Thiosemicarbazones/pharmacology , Antineoplastic Agents/chemical synthesis , Cell Line, Tumor , Cisplatin/pharmacology , Coordination Complexes/chemical synthesis , Crystallography, X-Ray , Drug Screening Assays, Antitumor , Ferrous Compounds/chemical synthesis , Humans , Magnetic Resonance Spectroscopy , Metallocenes , Structure-Activity Relationship , Thiosemicarbazones/chemical synthesisABSTRACT
A series of 5-aryl-1,4-benzodiazepines with chloro- or fluoro-substituents in the second ring have been synthesized and their anti-inflammatory, myeloperoxidase and anticancer properties studied. The synthesized compounds showed potential anti-inflammatory and anticancer activities, which were enhanced in the presence of a chloro-substituent in the second ring of the 5-aryl-1,4- benzodiazepine.
