Synthesis and in vitro anticancer and anti-HIV evaluation of new 2-mercaptobenzenesulfonamides.
The reactions of 6-chloro-3-methylthio-1,4,2-benzodithiazine 1,1-dioxide derivatives with appropriate diamines were investigated. Depending on the reaction conditions 2-mercaptobenzenesulfonamide derivatives or their oxidation product disulfides were obtained. All the compounds were tested at the US National Cancer Institute (Bethesda) for their in vitro anticancer and anti-HIV activities. The highest sensibility against leukemia cell lines was found for bis[2-(6-chloro-4-phenyl-3,4-dihydroquinazolin-2-yl)aminosulfonyl-5-chloro-4-(4-R2-phenylcarbamoyl)phenyl]disulfides (R2 = H or Cl). The results of anti-HIV tests displayed moderate activity of N-(pirydo[3,2-d]imidazol-2-yl)-2-mercaptobenzenesulfonamide.
Pomarnacka
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Department of Chemical Technology of Drugs, Medical University of Gdańsk, Poland. zopom@farmacja.amg.gda.pl
Kornicka
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A
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005260:Female; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D007928:Lethal Dose 50; D008297:Male; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014407:Tumor Cells, Cultured / Q000187:drug effects
D019380:Anti-HIV Agents; D000970:Antineoplastic Agents; D013438:Sulfhydryl Compounds; D013449:Sulfonamides