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dc.contributor.author
Garro, Hugo Alejandro
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dc.contributor.author
Pungitore, Carlos Rodolfo
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dc.date.available
2018-12-04T19:01:16Z
dc.date.issued
2015-08
dc.identifier.citation
Garro, Hugo Alejandro; Pungitore, Carlos Rodolfo; Coumarins as potential inhibitors of DNA polymerases and reverse transcriptases. searching new antiretroviral and antitumoral drugs; Bentham Science Publishers B.V.; Current Drug Discovery Technologies; 12; 2; 8-2015; 66-79
dc.identifier.issn
1875-6220
dc.identifier.uri
http://hdl.handle.net/11336/65769
dc.description.abstract
Human Immunodeficiency Virus (HIV) is the viral agent of Acquired Immunodeficiency Syndrome (AIDS), and at present, there is no effective vaccine against HIV. Reverse Transcriptase (RT) is an essential enzyme for retroviral replication, such as HIV as well as for other RNA infectious viruses like Human T lymphocyte virus. Polymerases act in DNA metabolism, modulating different processes like mitosis, damage repair, transcription and replication. It has been widely documented that DNA Polymerases and Reverse Transcriptases serve as molecular targets for antiviral and antitumoral chemotherapy. Coumarins are oxygen heterocycles that are widely distributed throughout the plant kingdom. Natural coumarins have attraction due to their bioactive properties such as tumor promotion inhibitory effects, and anti-HIV activity. Coumarins and derivates exhibit potent inhibitory effects on HIV-1 replication in lymphocytes and compounds isolated from Calophyllum inophyllum or DCK derivates showed inhibitory activity against human RT. Furthermore, natural isocoumarins isolated from cultures of fungi or hydroxycoumarins were able to inhibit human DNA polymerase. In view of their importance as drugs and biologically active natural products, and their medicinally useful properties, extensive studies have been carried out on the synthesis of coumarin compounds in recent years. Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs), a class of antiretroviral chemotherapeutic agents, act by binding to an allosteric pocket showing, generally, low toxicity. This work tries to summarize the investigation about natural and synthetic coumarins with the ability to inhibit key enzymes that play a crucial role in DNA metabolism and their possible application as antiretroviral and antitumoral agents.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Bentham Science Publishers B.V.
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
Cancer
dc.subject
Coumarins
dc.subject
Dna Polymerase
dc.subject
Hiv
dc.subject
In Silico
dc.subject
Inhibitors
dc.subject
Reverse Transcriptase
dc.subject.classification
Otras Ciencias Químicas
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dc.subject.classification
Ciencias Químicas
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dc.subject.classification
CIENCIAS NATURALES Y EXACTAS
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dc.title
Coumarins as potential inhibitors of DNA polymerases and reverse transcriptases. searching new antiretroviral and antitumoral drugs
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2018-09-20T13:14:02Z
dc.journal.volume
12
dc.journal.number
2
dc.journal.pagination
66-79
dc.journal.pais
Emiratos Árabes Unidos
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dc.description.fil
Fil: Garro, Hugo Alejandro. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto de Investigaciones en Tecnología Química. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia. Instituto de Investigaciones en Tecnología Química; Argentina
dc.description.fil
Fil: Pungitore, Carlos Rodolfo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto de Investigaciones en Tecnología Química. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia. Instituto de Investigaciones en Tecnología Química; Argentina
dc.journal.title
Current Drug Discovery Technologies
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/https://dx.doi.org/10.2174/1570163812666150716111719
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://www.eurekaselect.com/133277/article
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