Phosphine derivatives of ciprofloxacin and norfloxacin, a new class of potential therapeutic agents

被引：33

作者：

Bykowska, Aleksandra ^{[1
]}

Starosta, Radoslaw ^{[1
]}

Komarnicka, Urszula K. ^{[1
]}

Ciunik, Zbigniew ^{[1
]}

Kyziol, Agnieszka ^{[2
]}

Guz-Regner, Katarzyna ^{[3
]}

Bugla-Ploskonska, Gabriela ^{[3
]}

Jezowska-Bojczuk, Malgorzata ^{[1
]}

机构：

[1] Univ Wroclaw, Fac Chem, PL-50383 Wroclaw, Poland

[2] Jagiellonian Univ, Fac Chem, PL-30060 Krakow, Poland

[3] Univ Wroclaw, Inst Genet & Microbiol, Dept Microbiol, PL-51148 Wroclaw, Poland

来源：

NEW JOURNAL OF CHEMISTRY | 2014年 / 38卷 / 03期

关键词：

ELECTRON-DIFFRACTION; MOLECULAR-STRUCTURES; BIOLOGICAL-ACTIVITY; IODIDE COMPLEXES; SELENIDE; CRYSTAL; TRIPHENYLPHOSPHINE; SULFIDE; LIGANDS; OXIDE;

D O I：

10.1039/c3nj01243c

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

In this paper a new series of chalcogenides of diphenylmethylaminophosphine derived from ciprofloxacin (PPh2CH2Cp) 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.

引用

页码：1062 / 1071

页数：10

共 46 条

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