Synthesis of 1-(6-chloro-1,1-dioxo-1,4,2-benzodithiazin-3-yl)semi-carbazides and their transformation into 4-chloro-2-mercapto-N-(4,5-dihydro-5-oxo-4-phenyl-1H-1,2,4-triazol-3-yl)benzenesulfonamides as potential anticancer and anti-HIV agents.
Synthesis of a series of 1-(6-chloro-1,1-dioxo-1,4,2-benzodithiazin-3-yl)semicarbazides (6-16) and 4-chloro-2-mercapto-N-(4,5-dihydro-5-oxo-4-phenyl-1H-1,2,4-triazol-3-yl)benzenesulfonamides (17-22) were reported. Compounds 7-9, 17, 19-22 were tested at the US National Cancer Institute for their in vitro anticancer and anti-HIV activities. Results of anticancer screening showed moderate activity of 21 and 22, while 19 was found to have encouraging anti-HIV activity at EC(50) = 28.8 microM.
Pomarnacka
Elzbieta
E
Department of Chemical Drug Technology, Medical University of Gdañsk, 107 Gen. J. Hallera Str., 80-416 Gdañsk, Poland. zopom@farmacja.amg.gda.pl
Kozlarska-Kedra
Iwona
I
D019380:Anti-HIV Agents / Q000737:chemistry* / Q000493:pharmacokinetics; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D001711:Biotransformation; D002460:Cell Line; D006801:Humans; D012663:Semicarbazides / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D000096926:Benzenesulfonamides
D019380:Anti-HIV Agents; D000970:Antineoplastic Agents; D012663:Semicarbazides; D013449:Sulfonamides; D000096926:Benzenesulfonamides