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一些具有潜在抗癌或抗艾滋病毒活性的新型4-氯-2-巯基-N(4H-1,2,4-三唑-3-基)苯磺酰胺的合成

Syntheses of some new 4-chloro-2-mercapto-N(4H-1,2,4-triazol-3-yl) benzenesulphonamide with potential anticancer or anti-HIV activity.

作者信息

Sławiński J

机构信息

Department of Chemical Drug Technology, Medical University of Gdańsk, Poland.

出版信息

Acta Pol Pharm. 1997 Nov-Dec;54(6):461-6.

PMID:9604695
Abstract

4-Chloro-2-mercapto-5-R1-N-(4-R2-4H-1,2,4-triazol-3-yl) benzenesulphonamide [VIII-XIV] were prepared from the corresponding 4-chloro-3(R2-amino)-5-R1-1,1-dioxo-1,4, 2-benzodithiazines [I-VII] then compd. [VIII-X] were S-carboxyalkylated to the corresponding 2-¿5-chloro-4-methyl-2-[4-R2-4H-1,2,4-triazol-3-yl)aminosulphon yl] phenylthio¿alkanoic acids [XVII-XXVI]. Preliminary screening of anti HIV-1 and anticancer activity of compd. [XI,XII,XVII] was conducted.

摘要

4-氯-2-巯基-5-R1-N-(4-R2-4H-1,2,4-三唑-3-基)苯磺酰胺[VIII-XIV]由相应的4-氯-3(R2-氨基)-5-R1-1,1-二氧代-1,4,2-苯并二硫嗪[I-VII]制备,然后将化合物[VIII-X]进行S-羧烷基化反应,得到相应的2-[5-氯-4-甲基-2-[4-R2-4H-1,2,4-三唑-3-基)氨基磺酰基]苯硫基]链烷酸[XVII-XXVI]。对化合物[XI、XII、XVII]的抗HIV-1和抗癌活性进行了初步筛选。

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