Design and synthesis of ring C opened analogues of α-santonin as potential anticancer agents

dc.contributor.authorKhazir, Jabeena
dc.contributor.authorMir, Bilal Ahmad
dc.contributor.authorPilcher, Lynne A.
dc.contributor.authorRiley, Darren Lyall
dc.contributor.authorChashoo, Gousia
dc.contributor.authorIslam, Md Ataul
dc.contributor.authorSaxena, Ajit K.
dc.contributor.authorKumar, H.M.S. (Halmuthur Mahabalarao Sampath)
dc.date.accessioned2017-03-03T06:22:48Z
dc.date.issued2016-09
dc.description.abstractHere we describe ring opening reaction of a novel halo triene derivative viz., (3S, 5aS)-8- chloro-3a, 4, 5, 5a-tetrahydro-3, 5a, 9-trimethylnaphtho [1, 2-b] furan-2(3H)-one of α- santonin upon nucleophillic attack with alcohols. Halo-triene was synthesized from α- santonin upon reaction with vilsmeier reagent. The synthesised compounds from ring opening reaction were evaluated for anticancer activity against a panel of four human cancer cell lines (A-549, THP-1, HCT-15, and IMR-13). Most of the compounds exhibited promising anticancer activity against all cancer cells in vitro; however compound. 3d with benzyl substitution showed most potent anticancer activity with an IC50 value of 0.3 μM, 0.51 μM, 0.6 μM and 0.23 μM against A-549, THP-1, HCT- 116 and IMR-13 cell lines respectively.en_ZA
dc.description.departmentChemistryen_ZA
dc.description.departmentChemical Pathology
dc.description.departmentGenetics
dc.description.embargo2017-09-30
dc.description.librarianhb2017en_ZA
dc.description.urihttp://link.springer.com/journal/44en_ZA
dc.identifier.citationKhazir, J., Mir, B.A., Pilcher, L.A., Riley, D.L., Gashoo, G., Islam, M.A., Saxena, A.K. & Kumar, H.M.S. Design and synthesis of ring C opened analogues of α-santonin as potential anticancer agents. Medicinal Chemistry Research (2016) 25: 2030-2041. doi:10.1007/s00044-016-1633-8.en_ZA
dc.identifier.issn1054-2523 (print)
dc.identifier.issn1554-8120 (online)
dc.identifier.other10.1007/s00044-016-1633-8
dc.identifier.urihttp://hdl.handle.net/2263/59252
dc.language.isoenen_ZA
dc.publisherSpringeren_ZA
dc.rights© Springer Science+Business Media New York 2016. The original publication is available at : http://link.springer.comjournal/44.en_ZA
dc.subjectα-Santoninen_ZA
dc.subjectVilsmeier reactionen_ZA
dc.subjectAliphatic alcoholsen_ZA
dc.subjectCytotoxicityen_ZA
dc.titleDesign and synthesis of ring C opened analogues of α-santonin as potential anticancer agentsen_ZA
dc.typePostprint Articleen_ZA

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