Table 1.

Antiproliferative activity of DHIQs against DU-145 human prostate cancer cells and MDA MB-231 human breast cancer cells in vitro

Compd							GI50 [μm][a]
	R1	X	R2	R3	R4	R5	DU-145	MDA MB-231
8 a	H	CH2	OMe	H	H	H	>100	ND[b]
9 a	SO2NH2	CH2	OMe	H	H	H	>100	ND[b]
8 b	H	CH2	H	OMe	H	H	>100	ND[b]
9 b	SO2NH2	CH2	H	OMe	H	H	>100	ND[b]
8 c	H	CH2	H	H	OMe	H	>100	ND[b]
9 c	SO2NH2	CH2	H	H	OMe	H	>100	ND[b]
7 d	Bn	CH2	H	OMe	H	OMe	>100	ND[b]
8 d	H	CH2	H	OMe	H	OMe	>100	ND[b]
9 d	SO2NH2	CH2	H	OMe	H	OMe	>100	ND[b]
7 e	Bn	CH2	H	OMe	OMe	OMe	>100	ND[b]
8 e	H	CH2	H	OMe	OMe	OMe	>100	ND[b]
9 e	SO2NH2	CH2	H	OMe	OMe	OMe	>100	ND[b]
10 a	Bn	SO2	OMe	H	H	H	>100	>100
11 a	H	SO2	OMe	H	H	H	>100	13.4
12 a	SO2NH2	SO2	OMe	H	H	H	>100	>100
10 b	Bn	SO2	H	OMe	H	H	>100	>100
11 b	H	SO2	H	OMe	H	H	>100	>100
12 b	SO2NH2	SO2	H	OMe	H	H	>100	>100
11 c	H	SO2	H	H	OMe	H	>100	>100
12 c	SO2NH2	SO2	H	H	OMe	H	>100	>100
10 d	Bn	SO2	H	Cl	H	H	>100	>100
11 d	H	SO2	H	Cl	H	H	>100	>100
12 d	SO2NH2	SO2	H	Cl	H	H	>100	>100
11 e	H	SO2	CO2Me	H	H	H	>100	>100
12 e	SO2NH2	SO2	CO2Me	H	H	H	>100	13
15 a	Bn	CO	OMe	H	H	H	>100	43.6
16 a	H	CO	OMe	H	H	H	6.42	5.6
17 a	SO2NH2	CO	OMe	H	H	H	9.1	7.1
16 b	H	CO	H	OMe	H	H	3.63	1.89
17 b	SO2NH2	CO	H	OMe	H	H	5.3	3.5
15 c	Bn	CO	H	CN	H	H	>100	>100
16 c	H	CO	H	CN	H	H	70	37.4
17 c	SO2NH2	CO	H	CN	H	H	25	>100
15 d	Bn	CO	H	H	OMe	H	>100	ND[b]
16 d	H	CO	H	H	OMe	H	>100	ND[b]
17 d	SO2NH2	CO	H	H	OMe	H	>100	ND[b]
15 e	Bn	CO	H	OMe	OMe	H	>100	ND[b]
16 e	H	CO	H	OMe	OMe	H	2.39	1.6
17 e	SO2NH2	CO	H	OMe	OMe	H	3.4	2.08
15 f	Bn	CO	H	OMe	H	OMe	>100	ND[b]
16 f	H	CO	H	OMe	H	OMe	0.215	0.161
17 f	SO2NH2	CO	H	OMe	H	OMe	0.179	0.118
15 g	Bn	CO	H	OMe	OMe	OMe	>100	77.5
16 g	H	CO	H	OMe	OMe	OMe	0.051	0.071
17 g	SO2NH2	CO	H	OMe	OMe	OMe	0.166	0.275

[a] Results are the mean of three determinations. [b] Not determined.