期刊
CHINESE JOURNAL OF CHEMISTRY
卷 30, 期 8, 页码 1831-1840出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cjoc.201100668
关键词
nitrogen mustard; thiophene; antibacterial; antifungal; cytotoxicity
资金
- National Natural Science Foundation of China [21172181]
- key program from Natural Science Foundation of Chongqing [CSTC2012jjB10026]
- Specialized Research Fund for the Doctoral Program of Higher Education of China [SRFDP 20110182110007]
- Research Funds for the Central Universities [XDJK2011D007, XDJK2012B026]
The thiophene-derived amido bis-nitrogen mustard N2,N2,N5,N5-tetrakis(2-chloroethyl)-3,4-dimethylthiophene-2,5-dicarboxamide was designed and synthesized via five-step reactions from commercially available 2-chloroacetonitrile. This target compound was confirmed by 1H NMR, 13C NMR, MS, IR spectra and elemental analyses, and its structure was further characterized by X-ray single-crystal analysis. The biological activities for the title compound and some intermediates were evaluated in vitro for their antibacterial, antifungal and cytotoxic activities. The preliminary results showed that the title compound could inhibit efficiently the growth of the tested microorganisms including drug-resistant bacteria MRSA to some extent. Moreover, the target compound was found to be effective against prostatic carcinoma cell line (PC-3), breast carcinoma cell line (MCF-7), colon carcinoma (LoVo) and lung cancer (A549). Especially, it gave selective antitumor efficacy against prostatic carcinoma cell line (PC-3) at a low dose.
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