129696-75-9Relevant academic research and scientific papers
Cell death triggered by synthetic flavonoids in human leukemia cells is amplified by the inhibition of extracellular signal-regulated kinase signaling
Rubio, Sara,Leon, Francisco,Quintana, Jose,Cutler, Stephen,Estevez, Francisco
, p. 284 - 296 (2012/11/07)
A new class of methyl esters of flavonoids, with different substituents on the B ring were synthesized and evaluated for their antiproliferative activity against the human leukemia cell line HL-60. The presence of either a methyl group (1f) or a chlorine atom (1o) at position 2′ of the B ring played an important role in affecting antiproliferative activity. The cytotoxic effects of these compounds were accompanied by the concentration- and time-dependent appearance of DNA- and nuclear-fragmentation, increase in the percentage of sub-G1 cells, and processing of multiple caspases and poly(ADP-ribose)polymerase cleavage. Pretreatment of cells with the specific mitogen-activated extracellular kinases (MEK) 1/2 inhibitor PD98059, together with 1f and 1o, resulted in an important enhancement of cell death, which might have clinical implications for the use of both compounds in combination with MEK 1/2 inhibitors as potential therapeutic agents.
FURAN o-AMINONITRILES AS PRECURSORS TO FLAVONE ANALOGUES
Cutler, Stephen J.,El-Kabbani, Fiesal M.,Keane, Charlene,Fisher-Shore, Sherri L.,Blanton, C. DeWitt
, p. 651 - 661 (2007/10/02)
A procedure utilizing furan o-aminonitriles as precursors in the synthesis of substituted flavone analogues is reported.The key intermediates, o-hydroxyacetophenones, are obtained by a Diels-Alder reaction between the furans and methyl vinyl ketone.
