Synthesis of new pyrazolo[3,4-d]pyrimidine derivatives and evaluation of their anti-inflammatory and anticancer activities

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dc.contributor.author Abd El Razik, Heba A.
dc.contributor.author Mroueh, Mohamad
dc.contributor.author Faour, Wissam H.
dc.contributor.author Shebaby, Wassim N.
dc.contributor.author Daher, Costantine F.
dc.contributor.author Ashour, Hayam M. A.
dc.contributor.author Ragab, Hanan M.
dc.date.accessioned 2017-03-14T12:15:18Z
dc.date.available 2017-03-14T12:15:18Z
dc.date.copyright 2017 en_US
dc.date.issued 2017-03-14
dc.identifier.issn 1747-0277 en_US
dc.identifier.uri http://hdl.handle.net/10725/5366
dc.description.abstract This study reports the synthesis of two series of new purine bioisosteres comprising a pyrazolo[3,4-d]pyrimidine scaffold linked to piperazine moiety through different amide linkages. The newly synthesized compounds were evaluated for anticancer activity against four cell lines (MDA-MB-231, MCF-7, SF-268, B16F-10) and cyclooxygenase (COX-2) protein expression inhibition in lipopolysaccharide (LPS)-activated rat monocytes. The results revealed that most of the synthesized compounds showed moderate-to-high cytotoxic activity against at least one cell line, with compound 10b being the most active against all used cell lines (IC50 values 5.5–11 μg/ml) comparable to cisplatin. In addition, six of these compounds (7b, 10a–d, and 12c) demonstrated inhibition of LPS-induced COX-2 protein expression at low concentration (25 μg/ml) as compared to the control non-stimulated cells and showed a COX-2 selectivity index range comparable to diclofenac sodium. The overall results indicate that many of these pyrazolopyrimidine derivatives possess in vitro anti-inflammatory and anticancer activities at varying doses, and the most active compounds will be subjected to in vivo pharmacological evaluation. en_US
dc.language.iso en en_US
dc.title Synthesis of new pyrazolo[3,4-d]pyrimidine derivatives and evaluation of their anti-inflammatory and anticancer activities en_US
dc.type Article en_US
dc.description.version Published en_US
dc.author.school SAS en_US
dc.author.school SOM
dc.author.school SOP
dc.author.idnumber 199590020 en_US
dc.author.idnumber 200904962 en_US
dc.author.idnumber 201408580 en_US
dc.author.idnumber 199190130
dc.author.department Natural Sciences en_US
dc.description.embargo N/A en_US
dc.relation.journal Chemical biology & drug design en_US
dc.journal.volume 90
dc.journal.issue 1
dc.article.pages 83-96
dc.keywords Antineoplastic agents en_US
dc.keywords Inflammation en_US
dc.keywords Purine bioisosteres en_US
dc.keywords COX-2 en_US
dc.identifier.doi http://dx.doi.org/10.1111/cbdd.12929 en_US
dc.identifier.ctation Abd El Razik, H. A., Mroueh, M., Faour, W. H., Shebaby, W. N., Daher, C. F., Ashour, H., & Ragab, H. M. (2017). Synthesis of new pyrazolo [3, 4‐d] pyrimidine derivatives and evaluation of their anti‐inflammatory and anticancer activities. Chemical Biology & Drug Design 90 (1), 83-96 en_US
dc.author.email mmroueh@lau.edu.lb en_US
dc.author.email wissam.faour@lau.edu.lb en_US
dc.author.email wassim.shebaby@lau.edu.lb en_US
dc.author.email cdaher@lau.edu.lb
dc.identifier.tou http://libraries.lau.edu.lb/research/laur/terms-of-use/articles.php en_US
dc.identifier.url http://onlinelibrary.wiley.com/doi/10.1111/cbdd.12929/full en_US
dc.orcid.id https://orcid.org/0000-0003-1572-7133 en_US
dc.orcid.id https://orcid.org/0000-0002-0746-3687 en_US
dc.orcid.id https://orcid.org/0000-0002-8275-7263 en_US
dc.orcid.id https://orcid.org/0000-0002-9782-1870 en_US
dc.author.affiliation Lebanese American University en_US

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