当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis, anti-HIV-1 integrase, and cytotoxic activities of 4-chloro-N-(4-oxopyrimidin-2-yl)-2-mercaptobenzenesulfonamide derivatives.

Synthesis, anti-HIV-1 integrase, and cytotoxic activities of 4-chloro-N-(4-oxopyrimidin-2-yl)-2-mercaptobenzenesulfonamide derivatives.

Abstract：

:Several 4-chloro-N-(4-oxopyrimidin-2-yl)-2-mercaptobenzenesulfonamide derivatives 13-28 and 35-44 have been synthesized and tested as potential HIV-1 integrase (IN) inhibitors. Compounds 15-17, 19, 21-28, 36 and 41 inhibited IN with IC(50) values in the range of 3.3-63.0 microM. The compounds 13, 15, 16, 21-24 and 26-28 were further tested at the US National Cancer Institute for their in vitro activity against a panel of 53-57 human tumor cell lines. The compounds 26-28 were inactive, whereas the other compounds exhibited high or reasonable activity (GI(50)<0.01-20.0 microM) against one or more human tumor cell lines.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Brzozowski Z,Sławiński J,Saczewski F,Sanchez T,Neamati N

doi

10.1016/j.ejmech.2007.08.013

subject

Has Abstract

pub_date

2008-06-01 00:00:00

pages

1188-98

issue

6

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(07)00337-6

journal_volume

43

pub_type

杂志文章

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