Synthesis of 2-(4-Chloro-2-mercaptobenzenesulfonyl)-3,5-dihydroxy-1,1-dioxo-2H-1,2,4,6-thiatriazine Derivatives with Potential Anti-HIV and Anticancer Activities

• Autorzy: Brzozowski Z. , Sławiński J.
• Języki publikacji: EN

Abstrakty

EN

Several 2-(4-chloro-2-mercapto-5-R-benzenesulfonyl)-3,4-dihydroxy-1,1-dioxo-2H- 1,2,4,6-thiatriazines (9–12) have been synthesized as potential anti-HIV (9–10) or anticancer (11–12) agents. The in vitro anti-HIV or antitumor activities were tested at theUSNational Cancer Institute (Bethesda,MD), and the structure-activity relationships are discussed. Compound 9 (R =Me) showed good anti-HIV activity with 50% effective concentration (EC50) value of 73.2 ěMand moderate cytotoxic effect (IC50= 220.0 miM). The compounds 11 and 12 exhibited high or reasonable activity against most (98%) of the human tumor cell lines tested. Compound 12 (R = 4-ClC6H4NHCO) is theprominent of the compounds due to its good activity against 54 human tumor cell lines (GI50 = 0.67–38.9 ěM), and remarkable selectivity toward renal cancer RXF 393 cell line (GI50 = 0.67 miM).

Słowa kluczowe

EN

2-(4-chloro-2-mercapto-5-R-benzenesulfonyl)-3,4-dihydroxy-1,1-dioxo2H-1,2,4,6-thiatriazines; synthesis; anti-HIV and antitumor activities; structure-activity relationship

• Wydawca: Polskie Towarzystwo Chemiczne
• Czasopismo: Polish Journal of Chemistry
• Rocznik: 2007
• Tom: Vol. 81, nr 8
• Strony: 1419--1426
• Opis fizyczny: Bibliogr. 35 poz., rys.

Twórcy

autor

Brzozowski Z.

autor

Sławiński J.

• Department of Chemical Technology of Drugs, Medical University of Gdańsk, Al. Gen. J. Hallera 107, 80-416Gdańsk, Poland,

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