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Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment

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BIOORGANIC & MEDICINAL CHEMISTRY
卷 16, 期 2, 页码 794-809

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.10.034

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Diverse N-substituted anilines bearing hetaryl fragments were easily prepared from corresponding aldimines derived from commercially available aromatic aldehydes and anilines. 2-Furyl substituted anilines showed very good antifungal activities against dermatophytes, particularly against Trichophyton rubrum (MIC = 3.12-6.25 mu g/mL). In addition, all active compounds, 45-47, 73, and 74, were tested for cytotoxic activities against breast (MCF-7), lung (H-460), and central nervous system (SF-268) human cancer cell lines with the NCI-anticancer-drug screen. The activity of amines described in this paper, along with the low toxicity of most of them, shows promise for the future development of non-toxic new antimycotic agents. (c) 2007 Elsevier Ltd. All rights reserved.

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