Halogenated isoniazid derivatives as possible antitubercular and antineoplastic agents. Note 1.
Halogenated arylhydrazones, 2-aryl-4-thiazolidinones and their 1,1-dioxides containing isoniazid (INI) moieties were prepared and explored for antimicrobial (against bacteria, Candida and mycobacteria) and antitumor activities. None of the tested compounds showed any marked antimicrobial effect. Furthermore, among the compounds submitted to NCI in vitro primary antitumor screening, those bearing 3-fluoro or -chlorophenyl substituents were found to possess selective inhibitory effects on the growth of non small cell lung cancer, whereas those with para-phenyl substituents displayed selective effects, sometimes statistically significant, against leukemias.
Vigorita
M G
MG
Dipartimento Farmaco-Chimico, Facoltà di Farmacia, Università di Messina.
Basile
M
M
Zappalà
C
C
Gabbrielli
G
G
Pizzimenti
F
F
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D007538:Isoniazid / Q000031:analogs & derivatives* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests
D000970:Antineoplastic Agents; D000995:Antitubercular Agents; D007538:Isoniazid