SYNTHESIS AND HIV-1 REVERSE TRANSCRIPTASE INHIBITION ACTIVITY OF 1,4-NAPHTHOQUINONE DERIVATIVES

被引：17
|
作者：
Mahapatra, Anita [1 ]
Tshikalange, T. E. [2 ]
Meyer, J. J. M. [2 ]
Lall, Namrita [2 ]
机构：
[1] BV Patel PERD Ctr, Natl Inst Pharmaceut Educ & Res NIPER, Dept Nat Prod, Ahmadabad 380054, Gujarat, India
[2] Univ Pretoria, Fac Nat & Agr Sci, Dept Plant Sci, ZA-0002 Pretoria, South Africa
来源：
CHEMISTRY OF NATURAL COMPOUNDS | 2012年 / 47卷 / 06期
关键词：
HIV-1 reverse transcriptase; anti-HIV activity; cytotoxic activity; 1,4-napthoquinone; 7-methyljuglone; diospyrin; isodiospyrin; dimer; E; natalensis; EXTRACTS;
D O I：
10.1007/s10600-012-0094-7
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Some 1,4-napthoquinone derivatives were synthesized, and dimers of 5-hydroxy-7-methyl-1,4-naphthoquinone (5) were isolated from the roots of Euclea natalensis. Their structures were confirmed by spectroscopic (UV, IR, NMR, and MS) analysis. The HIV-1 reverse transcriptase inhibition activity of the compounds against recombinant HIV-1 enzyme was studied in vitro (non-radioactive HIV-RT colorimetric assay) using the Roche Diagnostic kit and compared with that of doxorubicin as standard drug. Some of the synthesized compounds exhibited exceptionally potent (91-100%) HIV-1 RT inhibition at 100 mu g/mL concentration. Surprisingly the dimers showed very weak activity.
引用
收藏
页码：883 / 887
页数：5
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