Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols

被引：46

作者：

Chauthe, Siddheshwar K. ^{[2
]}

Bharate, Sandip B. ^{[2
]}

Sabde, Sudeep ^{[1
]}

Mitra, Debashis ^{[1
]}

Bhutani, Kamlesh K. ^{[2
]}

Singh, Inder P. ^{[2
]}

机构：

[1] NCCS, Pune 411007, Maharashtra, India

[2] NIPER, Dept Nat Prod, Sas Nagar 160062, Punjab, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 05期

关键词：

Phloroglucinol; Anti-HIV activity; CEM-GFP cells; Antivirals; IN-VIVO; INHIBITORS; ANTIMALARIAL; EUGLOBALS;

D O I：

10.1016/j.bmc.2010.01.023

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Plants are an important source of a variety of bioactive compounds with different modes of action. Anti-HIV agents from plant sources can be useful in developing novel therapies for inhibiting HIV infection. Based on the reported anti-HIV activity of plant derived phloroglucinols, several new dimeric phloroglucinols were synthesized in the present study by varying substitution on aromatic ring and at methylene bridge. Some of the synthesized compounds have shown good HIV inhibitory activity in a human CD4+ T cell line (CEM-GFP) infected with HIV-1 NL4.3 virus isolate. Structure-activity studies indicate that phenyl, 4-benzyloxy-1-phenyl and cyclohexyl substitution at methylene bridge gave compounds with better anti-HIV activity. Compounds 22 and 24 showed highest anti-HIV activity with an IC50 of 0.28 mu M and 2.71 mu M, respectively, former was more active than the positive standard AZT in cell based assay. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：2029 / 2036

页数：8

共 29 条

[1]

[Anonymous], AIDS EP UPD

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