Synthesis and Inhibiting Activity of Some 4-Hydroxycoumarin Derivatives on HIV-1 Protease
Joint Authors
Argirova, Radka
Atanasov, Vasil
Genova-Kalou, Petia
Jensen, Frank
Hinkov, Anton
Manolov, Ilia
Stanchev, Stancho
Source
Issue
Vol. 2011, Issue 2011 (31 Dec. 2011), pp.1-9, 9 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2011-07-26
Country of Publication
Egypt
No. of Pages
9
Main Subjects
Pharmacy, Health & Medical Sciences
Pharmacology
Abstract EN
Six novel 4-hydroxycoumarin derivatives were rationally synthesized, verified, and characterized by molecular docking using crystal HIV-1 protease.
Molecular docking studies predicted antiprotease activity of (7) and (10).
The most significant functional groups, responsible for the interaction with HIV-1 protease by hydrogen bonds formation are pyran oxygen, atom, lactone carbonyl oxygen and one of the hydroxyl groups.
The newly synthesized compounds were biologically tested in MT-4 cells for inhibiting HIV-1 replication, exploring the protection of cells from the cytopathic effect of HIV measured by cell survival in MTT test.
One derivative −7 showed 76–78% inhibition of virus infectivity with IC50 = 0.01 nM, much less than the maximal nontoxic concentration (1 mM).
Antiprotease activity of 7 in two different concentrations was detected to be 25%.
Nevertheless, the results of study of (7) encourage using it as a pharmacophore for further synthesis and evaluation of anti-HIV activity.
American Psychological Association (APA)
Stanchev, Stancho& Jensen, Frank& Hinkov, Anton& Atanasov, Vasil& Genova-Kalou, Petia& Argirova, Radka…[et al.]. 2011. Synthesis and Inhibiting Activity of Some 4-Hydroxycoumarin Derivatives on HIV-1 Protease. ISRN Pharmaceutics،Vol. 2011, no. 2011, pp.1-9.
https://search.emarefa.net/detail/BIM-448684
Modern Language Association (MLA)
Stanchev, Stancho…[et al.]. Synthesis and Inhibiting Activity of Some 4-Hydroxycoumarin Derivatives on HIV-1 Protease. ISRN Pharmaceutics No. 2011 (2011), pp.1-9.
https://search.emarefa.net/detail/BIM-448684
American Medical Association (AMA)
Stanchev, Stancho& Jensen, Frank& Hinkov, Anton& Atanasov, Vasil& Genova-Kalou, Petia& Argirova, Radka…[et al.]. Synthesis and Inhibiting Activity of Some 4-Hydroxycoumarin Derivatives on HIV-1 Protease. ISRN Pharmaceutics. 2011. Vol. 2011, no. 2011, pp.1-9.
https://search.emarefa.net/detail/BIM-448684
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-448684