2-Mercapto-N-(azolyl)benzenesulphonamides. II. Syntheses, anti-HIV-1 and anticancer activity of some S-substituted 4-chloro-2-mercapto-5-methyl-N-(5-amino-1,2,4-triazol-3-yl) benzenesulphonamides.
The 4-chloro-2-mercapto-5-methyl-N-[5-R1-amino-S-triazol-3-yl] benzenesulphonamides (I-III; R1 = H, Ph or 3-MeOPh) were converted into S-substituted derivatives IV-XIV as potential anti-HIV-1 and/or anticancer agents. Preliminary screening data of compounds [IV-V, VII-XI] and [XIV] indicate that some of them exhibit weak anticancer activity [IV and XI] and moderate anti-HIV-1 activity [IV]. Some structure-activity relationships are also discussed.
Brzozowski
Z
Z
Department of Drug Technology, Faculty of Pharmacy, School of Medicine, Gdańsk, Poland.
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D006801:Humans; D007928:Lethal Dose 50; D010084:Oxidation-Reduction; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D019380:Anti-HIV Agents; D000970:Antineoplastic Agents; D013449:Sulfonamides