Antiviral and antiproliferative activity in vitro of some new benzimidazole derivatives.
The antiviral and antiproliferative activity of new compounds having n-benzenesulphony 1-2 (2 or 3-pyridylethyl) benzimidazole as a base structure were studied in vitro. Their antitumour activity against human chronic myeloid leukaemia cells was evaluated and compared with that of equimolar doses of daunorubicin. Only compound 7a, with the presence of both the pyridyl moiety bound at the ethylenic bridge in C-2 of benzimidazole and the nitro-group in the benzene ring, displays a selective antiproliferative effect against certain leukaemia cells and a good antiviral activity especially towards the Coxsackie B5 virus. However, it should be noted that, in the case of hydroxybenzyl-benzimidazole, resistance also builds up to compound 7a, the Coxsackie B5 virus developing resistance to it after about ten runs. Cytotoxicity tests show that many of these substances are well tolerated by the VERO cells. The mechanism of action is still unclear.
Castelli
M
M
Department of Biomedical Sciences, Section of Pharmacology, University of Modena and Reggio Emilia, Italy. Castma24@mail.unimo.it
Malagoli
M
M
Lupo
L
L
Riccomi
T R
TR
Casolari
C
C
Cermelli
C
C
Zanca
A
A
Baggio
G
G
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D000998:Antiviral Agents / Q000494:pharmacology*; D001562:Benzimidazoles / Q000494:pharmacology*; D002051:Burkitt Lymphoma / Q000188:drug therapy / Q000473:pathology; D002455:Cell Division / Q000187:drug effects; D002522:Chlorocebus aethiops; D003630:Daunorubicin / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004352:Drug Resistance, Microbial; D029822:Enterovirus B, Human / Q000187:drug effects; D006801:Humans; D015464:Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Q000188:drug therapy / Q000473:pathology; D054198:Precursor Cell Lymphoblastic Leukemia-Lymphoma / Q000188:drug therapy / Q000473:pathology; D014407:Tumor Cells, Cultured / Q000187:drug effects*; D014709:Vero Cells / Q000187:drug effects; D014780:Viruses / Q000187:drug effects*
D000970:Antineoplastic Agents; D000998:Antiviral Agents; D001562:Benzimidazoles; D003630:Daunorubicin