1. Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment.
- Author
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Kouznetsov VV, Vargas Méndez LY, Sortino M, Vásquez Y, Gupta MP, Freile M, Enriz RD, and Zacchino SA
- Subjects
- Drug Screening Assays, Antitumor, Humans, Imines chemistry, Microbial Sensitivity Tests, Molecular Structure, National Cancer Institute (U.S.), United States, Aniline Compounds chemical synthesis, Aniline Compounds chemistry, Aniline Compounds pharmacology, Antifungal Agents chemical synthesis, Antifungal Agents chemistry, Antifungal Agents pharmacology, Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology
- Abstract
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=3.12-6.25microg/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.
- Published
- 2008
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