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Please use this identifier to cite or link to this item: https://doi.org/10.1016/j.bmc.2009.11.065
DC FieldValue
dc.titleAntifolate and antiproliferative activity of 6,8,10-triazaspiro[4.5]deca-6,8-dienes and 1,3,5-triazaspiro[5.5]undeca-1,3-dienes
dc.contributor.authorMa, X.
dc.contributor.authorChui, W.-K.
dc.date.accessioned2014-10-09T06:43:31Z
dc.date.available2014-10-09T06:43:31Z
dc.date.issued2010-01-15
dc.identifier.citationMa, X., Chui, W.-K. (2010-01-15). Antifolate and antiproliferative activity of 6,8,10-triazaspiro[4.5]deca-6,8-dienes and 1,3,5-triazaspiro[5.5]undeca-1,3-dienes. Bioorganic and Medicinal Chemistry 18 (2) : 737-743. ScholarBank@NUS Repository. https://doi.org/10.1016/j.bmc.2009.11.065
dc.identifier.issn09680896
dc.identifier.urihttp://scholarbank.nus.edu.sg/handle/10635/88546
dc.description.abstractTwo series of triazaspiroalkanedienes, bearing a substituted phenoxy propyloxy side chain, were identified as potent mammalian DHFR inhibitors. One series has a 6,5-spiro bicyclic ring system and the other series has a 6,6-spiro bicyclic system. Both series were synthesized and tested for in vitro mammalian DHFR inhibitory activity and antiproliferative activity against A549 human lung-cancer cells. Compound 3c showed the highest antiproliferative activity against A549 cells with an IC50 value of 27.1 nM. Rescue experiment confirmed its antifolate antiproliferative mechanism. The excellent antifolate and antiproliferative activity of selected analogues presented in this study warrants further investigation as potential leads in the anticancer drug discovery. © 2009 Elsevier Ltd. All rights reserved.
dc.description.urihttp://libproxy1.nus.edu.sg/login?url=http://dx.doi.org/10.1016/j.bmc.2009.11.065
dc.sourceScopus
dc.subject1,3,5-Triazines
dc.subjectAntiproliferative activity
dc.subjectDHFR inhibitors
dc.subjectSpiro rings
dc.typeArticle
dc.contributor.departmentCHEMICAL & BIOMOLECULAR ENGINEERING
dc.contributor.departmentPHARMACY
dc.description.doi10.1016/j.bmc.2009.11.065
dc.description.sourcetitleBioorganic and Medicinal Chemistry
dc.description.volume18
dc.description.issue2
dc.description.page737-743
dc.description.codenBMECE
dc.identifier.isiut000273613500026
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