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Cell death triggered by synthetic flavonoids in human leukemia cells is amplified by the inhibition of extracellular signal-regulated kinase signaling.

Abstract：

: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-G(1) 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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Rubio S,León F,Quintana J,Cutler S,Estévez F

doi

10.1016/j.ejmech.2012.07.028

subject

Has Abstract

pub_date

2012-09-01 00:00:00

pages

284-96

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(12)00454-0

journal_volume

55

pub_type

杂志文章

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