2006
DOI: 10.1248/cpb.54.682
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HIV-1 Integrase Inhibition of Biscoumarin Analogues

Abstract: Nineteen biscoumarins bearing free and modified hydroxyl substituents at benzoyloxyphenyl linker have been synthesized by multiple step synthesis. Among these biscoumarins, thirteen were found to be active molecules against HIV-1 integrase (HIV-1 IN). The structure-activity relationship of the nineteen compounds on HIV IN may be useful for the design of potent therapeutic agents.

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Cited by 76 publications
(27 citation statements)
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“…It also represents the core structure of several molecules of pharmaceutical importance. Coumarin has been reported to serve as anti-cancer [2], anti-microbial [3], anti-inflammatory [4] and anticoagulant [5]. These pharmacological properties of coumarin encouraged us to synthesize some coumarin derivatives.…”
Section: Introductionmentioning
confidence: 99%
“…It also represents the core structure of several molecules of pharmaceutical importance. Coumarin has been reported to serve as anti-cancer [2], anti-microbial [3], anti-inflammatory [4] and anticoagulant [5]. These pharmacological properties of coumarin encouraged us to synthesize some coumarin derivatives.…”
Section: Introductionmentioning
confidence: 99%
“…17 Dicoumarol also potentiates cisplatin-induced apoptosis urogenital cancer cell lines. 18 Dicoumarol and its derivatives display wide range of pharmacological activity such as anti-HIV, 19,20 antibiotic, 21 antitumor and anti-inflammatory. 22 Dicoumarols are generally synthesized by cascade reaction of two equivalents of 4-hydroxycoumarin and different aldehydes.…”
Section: Introductionmentioning
confidence: 99%
“…Biscoumarins are a large group of heterocycles with diverse, interesting and important biological and pharmaceutical activities [1][2][3][4][5] activities. In recent years and because of these important activities, several methods are reported for the synthesis of biscoumarins using a variety of catalysts and reagents [6][7][8][9][10][11][12][13][14].…”
Section: Introductionmentioning
confidence: 99%