Co-reporter:Quang H. Luu, Shizue Mito
Tetrahedron 2015 Volume 71(Issue 6) pp:895-916
Publication Date(Web):11 February 2015
DOI:10.1016/j.tet.2014.11.008
Co-reporter:Diego A. Pedroza, Fernando De Leon, Armando Varela-Ramirez, Carolina Lema, Renato J. Aguilera, Shizue Mito
Bioorganic & Medicinal Chemistry 2014 Volume 22(Issue 2) pp:842-847
Publication Date(Web):15 January 2014
DOI:10.1016/j.bmc.2013.12.007
Here, we tested seven 2-acylated-1,4-hydronaphthoquinones for their cytotoxic effects on a panel of cancer lymphoma/leukemia cells and compared to a non-cancer origin cell line. Several naphthohydroquinones exhibited selective cytotoxic effects on lymphoma/leukemia cells with lowest activity on non-cancer cells. The mode of cell death induced by an acylated naphthohydroquinone, which has a long alkyl chain, was found to be via apoptosis. Furthermore, the naphthohydroquinone provoked mitochondria depolarization and activation of its downstream effector, caspase-3, thus implicating the intrinsic apoptotic pathway as its mechanism to exert cell death.The toxicity against leukemia/lymphoma CEM/Jurkat/Nalm-6/Ramos cells is: IC50 = 5.99/6.56/5.80/0.98 μM. Significant less cytotoxicity was exerted on non-cancerous Hs27 cells: IC50 = 43.75 μM. The death program was initiated via mitochondria depolarization, implicating the intrinsic apoptotic pathway. The progression of the apoptosis was confirmed by the activation of its downstream effector, caspase-3.
Co-reporter:Fernando De Leon, Sudhakar Kalagara, Ashley A. Navarro, Shizue Mito
Tetrahedron Letters 2013 Volume 54(Issue 24) pp:3147-3149
Publication Date(Web):12 June 2013
DOI:10.1016/j.tetlet.2013.04.021
Synthesis of acyl-5,8-quinolinediols using sunlight was investigated. Photo-Friedel–Crafts acylation of quinoline-5,8-dione and aldehyde afforded the corresponding 6-acyl-5,8-quinolinediols regioselectively in moderate to good yields. The compounds have a variety of potential applications.