Synthesis, characterization and anti-HIV and antitumor activities of new coumarin derivatives

被引：49

作者：

Al-Soud, Yaseen A. ^{[1
]}

Al-Sa'doni, Haitham H. ^{[1
]}

Amajaour, Houssain A. S. ^{[1
]}

Salih, Kifah S. M. ^{[2
]}

Mubarak, Mohammad S. ^{[2
]}

Al-Masoudi, Najim A. ^{[3
]}

Jaber, Ihsan H. ^{[1
]}

机构：

[1] Univ Al Al Bayt, Coll Sci, Dept Chem, Al Mafraq, Jordan

[2] Univ Jordan, Fac Sci, Dept Chem, Amman, Jordan

[3] Univ Konstanz, Fachbereich Chem, D-78457 Constance, Germany

来源：

ZEITSCHRIFT FUR NATURFORSCHUNG SECTION B-A JOURNAL OF CHEMICAL SCIENCES | 2008年 / 63卷 / 01期

关键词：

anti-HIV activity; antitumor activity; coumarins; imidazoles; NNRTIs;

D O I：

10.1515/znb-2008-0112

中图分类号：

O61 [无机化学];

学科分类号：

070301 [无机化学]; 081704 [应用化学];

摘要：

A new series of coumarin and benzofuran derivatives were synthesized as potential non-nucleoside reverse transcriptase inhibitors (NNRTIs) by reacting, separately, 4-bromomethylcoumarins, their sulphonyl chlorides, and ethyl 3-(bromomethyl)-6-methoxy-1-benzofuran-2-carboxylate with different imidazoles and their benzo analogs. The antiviral (HIV-1, HIV-2) properties of the newly synthesized compounds were investigated in vitro and all compounds were found to be inactive, except 10 which showed inhibition of HIV-2 with EC50 > 0.51 mu g mL(-1). The in vitro cytotoxicity of 17 and 19 was assayed against a panel of tumor cell lines consisting of CD4 human T-cells.

引用

页码：83 / 89

页数：7

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