Brzozowski Z
Department of Drug Technology, Faculty of Pharmacy, School of Medicine, Gdańsk, Poland.
Acta Pol Pharm. 1995 Jul-Aug;52(4):287-92.
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.
4-氯-2-巯基-5-甲基-N-[5-R1-氨基-S-三唑-3-基]苯磺酰胺(I-III;R1 = H、Ph或3-MeOPh)被转化为S-取代衍生物IV-XIV,作为潜在的抗HIV-1和/或抗癌药物。化合物[IV-V、VII-XI]和[XIV]的初步筛选数据表明,其中一些具有较弱的抗癌活性[IV和XI]以及中等的抗HIV-1活性[IV]。还讨论了一些构效关系。