129696-79-3Relevant academic research and scientific papers
Synthesis of flavone-8-carboxylic acid analogues as potential antitumor agents
Cutler,El-Kabbani,Keane,Fisher-Shore,McCabe,Johnson,DeWitt Blanton Jr.
, p. 407 - 414 (1993)
Furan o-aminonitriles may be utilized as precursors in the synthesis of flavone-8-carboxylic acids. Some results from in vivo evaluation against P388 leukemia, colon carcinoma 38, and B16 melanoma models suggest that selected examples of the acids are potentially as effective as the antitumor compound, flavone acetic acid. The flavone-8-carboxylic acids did not exhibit significant activity against an in vitro HIV screen or an in vitro antitumor screen consisting of a cell panel of 60 lines.
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.
