Women's Health Weekly
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Cancer Therapy
Piperazinobenzopyranones and phenalkylaminobenzopyranones inhibited ABCG2
February 9th, 2006
Piperazinobenzopyranones and phenalkylaminobenzopyranones could be used to inhibit breast cancer resistance protein (ABCG2). "In continuing research that led us to identify chromanone derivatives (J Med Chem 2003, 46, 2125) as P-glycoprotein inhibitors, we obtained analogues able to modulate multidrug resistance (MDR) mediated by the breast cancer resistance protein (BCRP). The linkage of 5-hydroxybenzopyran-4-one to piperazines or phenalkylainines affords highly potent inhibitors of BCRP. By using sensitive (HCT116) and resistant colon cancer cells expressing BCRP, we evaluated the effect of 14 benzopyranone (chromone) derivatives on the accumulation and the cytotoxic...
Source: Women's Health Weekly (2006-02-09)
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