A set of benzimidazole derivatives bearing on position 2 a tetrahydropyranyl or tetrahydrofuranyl residue was prepared and tested for antitumoral, anti HIV-1 and other pharmacological activities. While the anti-HIV activity was completely lacking, moderate antitumoral activity was found in a few compounds; particularly the 5,6-dichloro-2-(tetrahydropyran-2-yl)-benzimidazole (8) was able to inhibit the growth of 19 cell lines of humane tumors at near micromolar concentration. On the other hand compounds 4, 6-8 and 10 exhibited significant tracheal relaxant activity in vitro at concentration 3-10 micrograms/ml, thus resulting superior to theophylline and comparable to amrinone.
|Titolo:||Synthesis and biological investigations of 2-(tetrahydropyran-2'-yl) and 2-(tetrahydrofuran-2'-yl)benzimidazoles|
SPARATORE, ANNA CONCETTINA (Ultimo)
|Parole Chiave:||Animals; Drug Screening Assays, Antitumor; Anti-HIV Agents; Antineoplastic Agents; Guinea Pigs; Humans; Spectrophotometry, Ultraviolet; Mice; Furans; HIV-1; Magnetic Resonance Spectroscopy; Spectrophotometry, Infrared; Benzimidazoles; Muscle, Smooth; Pyrans; T-Lymphocytes|
|Settore Scientifico Disciplinare:||Settore CHIM/08 - Chimica Farmaceutica|
|Data di pubblicazione:||1997|
|Appare nelle tipologie:||01 - Articolo su periodico|