Table 3.

Inhibitory activities of compounds 45–59 against BCRP and P-gp as determined in the pheophorbide A and calcein AM assays.

Compound	Cell Line and Assay/IC50 1 (µM)			Cell Line/GI50 2		Ref.
	MDCK II BCRP Pheo. A	MDCK II BCRP Hoechst 33342	P-gp Overexpressing A2780adr Calcein AM	MDCK II Wild Type	BDCK II BCRP
45	1.30	-	0.42	3.42	5.14	[100]
46	0.60	-	0.48	12.60	10.90	[100]
47	0.84	-	2.34	-	-	[100]
48	0.29	-	18.8	3.46	4.80	[100]
49	0.19	-	14.9	132	92.9	[100]
50	2.18	-	-	-	-	[101]
51	1.30	-	-	7.88	7.08	[101]
52	0.98	0.50	-	17.40	20.50	[101]
53	0.97	0.57	0.49	69.30	65.90	[101]
54	0.60	0.50	-	89.40	93.20	[101]
55	-	0.22	1.13	80.00	78.00	[102]
56	-	0.88	-	-	-	[102]
57	1.97	-	-	7.56	9.38	[103]
58	6.33	-	-	-	-	[103]
59	3.37	-	-	18.90	27.7	[103]
Ko143 (9)	0.2	0.22	-	11.10	10.9	[100,101]
cyclosporine A (2)	-	-	1.41			[100]

¹ IC₅₀—Concentration producing 50% protein function inhibition. The efficiency of each chalcone derivative to inhibit substrate efflux from BCRP- or P-gp-overexpressing cells was determined by flow cytometry, relatively to control cells giving maximal substrate accumulation; The IC₅₀ values were determined by using increasing concentrations of test compounds. ² GI₅₀—Concentration of compound that inhibited cell growth by 50%, used to access intrinsic cytotoxicity of tested compounds determined by the MTT assay, using MDCK II BCRP and MDCK II wild-type cells.