Khazir, JabeenaMir, Bilal AhmadPilcher, Lynne A.Riley, Darren LyallChashoo, GousiaIslam, Md AtaulSaxena, Ajit K.Kumar, H.M.S. (Halmuthur Mahabalarao Sampath)2017-03-032016-09Khazir, 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/s00044-016-1633-8.1054-2523 (print)1554-8120 (online)10.1007/s00044-016-1633-8http://hdl.handle.net/2263/59252Here 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© Springer Science+Business Media New York 2016. The original publication is available at : http://link.springer.comjournal/44.α-SantoninVilsmeier reactionAliphatic alcoholsCytotoxicityPostprint Article