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 Faour, Wissam H.
dc.contributor.author Mroueh, Mohamad
dc.contributor.author Abd El Razik, Heba A.
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 2019-04-23T13:57:04Z
dc.date.available 2019-04-23T13:57:04Z
dc.date.copyright 2016 en_US
dc.date.issued 2019-04-23
dc.identifier.issn 1747-0285 en_US
dc.identifier.uri http://hdl.handle.net/10725/10496
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 SOM en_US
dc.author.idnumber 200904962 en_US
dc.author.department N/A en_US
dc.description.embargo N/A en_US
dc.relation.journal Chemical Biology & Drug Design en_US
dc.journal.volume 90 en_US
dc.journal.issue 1 en_US
dc.article.pages 83-96 en_US
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 https://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. M., & 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 wissam.faour@lau.edu.lb en_US
dc.identifier.tou http://libraries.lau.edu.lb/research/laur/terms-of-use/articles.php en_US
dc.identifier.url https://onlinelibrary.wiley.com/doi/full/10.1111/cbdd.12929 en_US
dc.author.affiliation Lebanese American University en_US

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