Mostrar el registro sencillo del ítem
dc.contributor.author
Channar, Pervaiz Ali
dc.contributor.author
Afzal, Saira
dc.contributor.author
Ejaz, Syeda Abida
dc.contributor.author
Saeed, Aamer
dc.contributor.author
Larik, Fayaz Ali
dc.contributor.author
Mahesar, Parvez Ali
dc.contributor.author
Lecka, Joanna
dc.contributor.author
Sévigny, Jean
dc.contributor.author
Erben, Mauricio Federico
![Se ha confirmado la validez de este valor de autoridad por un usuario](/themes/CONICETDigital/images/authority_control/invisible.gif)
dc.contributor.author
Iqbal, Jamshed
dc.date.available
2019-11-01T16:47:57Z
dc.date.issued
2018-08
dc.identifier.citation
Channar, Pervaiz Ali; Afzal, Saira; Ejaz, Syeda Abida; Saeed, Aamer; Larik, Fayaz Ali; et al.; Exploration of carboxy pyrazole derivatives: Synthesis, alkaline phosphatase, nucleotide pyrophosphatase/phosphodiesterase and nucleoside triphosphate diphosphohydrolase inhibition studies with potential anticancer profile; Elsevier France-editions Scientifiques Medicales Elsevier; European Journal of Medical Chemistry; 156; 8-2018; 461-478
dc.identifier.issn
0223-5234
dc.identifier.uri
http://hdl.handle.net/11336/87817
dc.description.abstract
In the present work we report the synthesis of new aryl pyrazole derivatives using 1,3-dicarbonyl motifs. The reaction was proceeded by the cyclization of pentane-2,4-dione (1a), 3-chloropentane-2,4-dione (1b) or ethyl 3-oxobutanoate (1c) with different aryl hydrazines. The products, which can be regarded as 1H-pyrazol-1-yl-one analogues (3a-f, 3g-o, 4a-c, 5a-b) and represent drug like molecules along with well-developed structure?activity relationships, were obtained in good to excellent yield. The structures of synthesized compounds were charcterized on the basis of FT-IR, 1H NMR, 13C NMR and mass spectroscopic data. Considering alkaline phosphatases (APs), nucleotide pyrophosphatases/phosphodiesterases (NPPs) and nucleoside triphosphate diphosphohydrolase as the molecular targets, the effects of these synthesized compounds were investigated on different isozymes of APs, NPPs and NTPDases. The data revealed that the synthesized compounds inhibited both enzymes but most of them inhibited tissue non-specific alkaline phosphatase (TNAP) more selectively. The antitumor activity results indicated that the synthesized derivatives have strong inhibitory effects on the growth of selected cell lines from different tissues such as breast, bone marrow and cervix (MCF-7, K-562 and Hela) but with varying intensities. Moreover the binding mode of interactions were explained on the basis of molecular docking and in-silico studies.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Elsevier France-editions Scientifiques Medicales Elsevier
![Se ha confirmado la validez de este valor de autoridad por un usuario](/themes/CONICETDigital/images/authority_control/invisible.gif)
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
ALKALINE PHOSPHATASES (APS)
dc.subject
ANTITUMOR ACTIVITY
dc.subject
HYDRAZIDES
dc.subject
NUCLEOTIDE PYROPHOSPHATASES (NPPS)
dc.subject
PYRAZOLES
dc.subject.classification
Otras Ciencias Químicas
![Se ha confirmado la validez de este valor de autoridad por un usuario](/themes/CONICETDigital/images/authority_control/invisible.gif)
dc.subject.classification
Ciencias Químicas
![Se ha confirmado la validez de este valor de autoridad por un usuario](/themes/CONICETDigital/images/authority_control/invisible.gif)
dc.subject.classification
CIENCIAS NATURALES Y EXACTAS
![Se ha confirmado la validez de este valor de autoridad por un usuario](/themes/CONICETDigital/images/authority_control/invisible.gif)
dc.title
Exploration of carboxy pyrazole derivatives: Synthesis, alkaline phosphatase, nucleotide pyrophosphatase/phosphodiesterase and nucleoside triphosphate diphosphohydrolase inhibition studies with potential anticancer profile
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2019-10-22T16:42:29Z
dc.journal.volume
156
dc.journal.pagination
461-478
dc.journal.pais
Francia
![Se ha confirmado la validez de este valor de autoridad por un usuario](/themes/CONICETDigital/images/authority_control/invisible.gif)
dc.description.fil
Fil: Channar, Pervaiz Ali. Quaid-i-azam University; Pakistán
dc.description.fil
Fil: Afzal, Saira. Comsats University Islamabad; Pakistán
dc.description.fil
Fil: Ejaz, Syeda Abida. Comsats University Islamabad; Pakistán
dc.description.fil
Fil: Saeed, Aamer. Quaid-i-azam University; Pakistán
dc.description.fil
Fil: Larik, Fayaz Ali. Quaid-i-azam University; Pakistán
dc.description.fil
Fil: Mahesar, Parvez Ali. Quaid-i-azam University; Pakistán. Shah Abdul Latif University; Pakistán
dc.description.fil
Fil: Lecka, Joanna. Laval University; Canadá
dc.description.fil
Fil: Sévigny, Jean. Laval University; Canadá
dc.description.fil
Fil: Erben, Mauricio Federico. Facultad de Ciencias Exactas, Universidad Nacional de la Plata; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Centro de Química Inorgánica "Dr. Pedro J. Aymonino". Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Centro de Química Inorgánica "Dr. Pedro J. Aymonino"; Argentina
dc.description.fil
Fil: Iqbal, Jamshed. Comsats University Islamabad; Pakistán
dc.journal.title
European Journal of Medical Chemistry
![Se ha confirmado la validez de este valor de autoridad por un usuario](/themes/CONICETDigital/images/authority_control/invisible.gif)
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.ejmech.2018.07.002
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S0223523418305580?via%3Dihub
Archivos asociados