Table 1.

Antiproliferative effects of acrylic acids 13–25 in MCF-7 human breast cancer cells ^a.

Compound	R1	R2	R3	R4	R5	R6	R7	IC50 (μM) b
13	COOH	H	OMe	OMe	OMe	OMe	OH	0.120
14	COOH	H	OMe	OMe	OMe	OMe	H	7.80
15	COOH	H	OMe	OMe	OMe	OMe	F	55.1
16	COOH	H	OMe	OMe	OMe	OMe	NH2	6.70
17	COOH	H	OMe	OMe	OMe	Br	H	>50
18	COOH	H	OMe	OMe	OMe	F	H	>50
19	COOH	H	OMe	OMe	OMe	Me	H	26.1
20	COOH	H	OMe	OMe	OMe	SMe	H	10.6
21	COOH	H	OMe	OMe	OMe	OMe	NO2	2.50
22	COOH	H	OMe	OMe	OMe	-C4H4-		15.3
23	H	COOH	OMe	OMe	OMe	OMe	H	>50
24	CO2Me	H	OMe	OMe	OMe	OMe	OH	2.80
25	H	COOH	-OCH2O-		H	OMe	H	>50
47	H	CO-Pi	OMe	OMe	OMe	OMe	H	> 50
48	H	CO-Py	OMe	OMe	OMe	OMe	H	>50
49	CO-Pi e	H	OMe	OMe	OMe	OMe	OH	>50
52	CO-Py f	H	OMe	OMe	OMe	OMe	H	>50
53	CO-Pi e	H	OMe	OMe	OMe	OMe	H	g
54	CO-Py f	H	OMe	OMe	OMe	OMe	NH2	>50
55	CO-Pi e	H	OMe	OMe	OMe	OMe	NH2	h
26 (CA4) c	H	H	OMe	OMe	OMe	OMe	OH	0.008
11 d	H	-	-	-	-	-	-	0.029
12	OH	-	-	-	-	-	-	0.028

^a Mean IC₅₀ values of compounds for their antiproliferative effects and percent cytotoxicity on a human MCF-7 breast cancer cell line. ^b IC₅₀ values are half maximal inhibitory concentrations required to block the growth stimulation of MCF-7 cells. Values are an average of at least three experiments performed in triplicate with typical standard errors below 15%. ^c The IC₅₀ value obtained for 26 (CA4) in this assay is 8 nM for MCF-7 and is in good agreement with the reported values for CA4 using the MTT assay on human MCF-7 breast cancer cell lines(see refs. [59,68,69]). ^d The reported IC₅₀ value for endoxifen in the MCF-7 cell line is 50 nM [70]. ^e Pi piperidine, ^f Py = pyrrole. ^g 35% growth inhibition for compound 53 at 10 μM. ^h 34% growth inhibition for compound 55 at 10 μM.