Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment.
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.
Kouznetsov
Vladímir V
VV
Laboratorio de Química Orgánica y Biomolecular, Escuela de Química, Universidad Industrial de Santander, A.A. 678, Bucaramanga, Colombia. kouznet@uis.edu.co
Vargas Méndez
Leonor Y
LY
Sortino
Maximiliano
M
Vásquez
Yelkaira
Y
Gupta
Mahabir P
MP
Freile
Mónica
M
Enriz
Ricardo D
RD
Zacchino
Susana A
SA
D000814:Aniline Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007097:Imines / Q000737:chemistry; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D054547:National Cancer Institute (U.S.); D014481:United States
D000814:Aniline Compounds; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D007097:Imines