Design and synthesis of ring C opened analogues of α-santonin as potential anticancer agents
dc.contributor.author | Khazir, Jabeena | |
dc.contributor.author | Mir, Bilal Ahmad | |
dc.contributor.author | Pilcher, Lynne A. | |
dc.contributor.author | Riley, Darren Lyall | |
dc.contributor.author | Chashoo, Gousia | |
dc.contributor.author | Islam, Md Ataul | |
dc.contributor.author | Saxena, Ajit K. | |
dc.contributor.author | Kumar, H.M.S. (Halmuthur Mahabalarao Sampath) | |
dc.date.accessioned | 2017-03-03T06:22:48Z | |
dc.date.issued | 2016-09 | |
dc.description.abstract | Here 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.department | Chemistry | en_ZA |
dc.description.department | Chemical Pathology | |
dc.description.department | Genetics | |
dc.description.embargo | 2017-09-30 | |
dc.description.librarian | hb2017 | en_ZA |
dc.description.uri | http://link.springer.com/journal/44 | en_ZA |
dc.identifier.citation | Khazir, 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.issn | 1054-2523 (print) | |
dc.identifier.issn | 1554-8120 (online) | |
dc.identifier.other | 10.1007/s00044-016-1633-8 | |
dc.identifier.uri | http://hdl.handle.net/2263/59252 | |
dc.language.iso | en | en_ZA |
dc.publisher | Springer | en_ZA |
dc.rights | © Springer Science+Business Media New York 2016. The original publication is available at : http://link.springer.comjournal/44. | en_ZA |
dc.subject | α-Santonin | en_ZA |
dc.subject | Vilsmeier reaction | en_ZA |
dc.subject | Aliphatic alcohols | en_ZA |
dc.subject | Cytotoxicity | en_ZA |
dc.title | Design and synthesis of ring C opened analogues of α-santonin as potential anticancer agents | en_ZA |
dc.type | Postprint Article | en_ZA |