Phosphine derivatives of ciprofloxacin and norfloxacin, a new class of potential therapeutic agentsElectronic supplementary information (ESI) available: Crystal packing pictures, detailed NMR data, the selected photos of the cells after treatment with the tested compounds and cytotoxic assay curves for all presented compounds. CCDC 948747 (OPCp·2CH3COCH3), 948748 (SPCp·0.5CH2Cl2) and 948749 (SePCp·0.79CH3OH·0.11H2O). For ESI and crystallographic data in CIF or other electronic format see DOI: 10

• Main Authors: Bykowska, Aleksandra, Starosta, Rados aw, Komarnicka, Urszula K, Ciunik, Zbigniew, Kyzio, Agnieszka, Guz-Regner, Katarzyna, Bugla-P osko ska, Gabriela, Je owska-Bojczuk, Ma gorzata
• Format: Article
• Language: English
• ISSN: 1144-0546; 1369-9261
• DOI: 10.1039/c3nj01243c

In this paper a new series of chalcogenides of diphenylmethylaminophosphine derived from ciprofloxacin (PPh 2 CH 2 Cp) and a new phosphine derived from norfloxacin (PPh 2 CH 2 Nr) are presented. The synthesized compounds were characterized by NMR, MS and X-ray techniques. Both phosphines exhibit antibacterial activity against: S. aureus , E. coli , K. pneumoniae and P. aeruginosa , similar to ciprofloxacin and norfloxacin. They inhibit the growth of microorganisms in relatively low concentrations. Chalcogenides are slightly less active than phosphines and unmodified antibiotics. All the derivatives were also tested in vitro as anticancer agents towards mouse colon carcinoma (CT26) and human lung adenocarcinoma (A549). Cytotoxicity studies revealed that phosphines and their chalcogenides are able to inhibit the proliferation of the cells at relatively low concentrations. Moreover, all the tested compounds are more active against tested cell lines than cisplatin - the main representative of antitumor drugs. Two diphenyl(aminomethyl)phosphines derived from ciprofloxacin and norfloxacin and a new series of their chalcogenides are presented.