Table 1. Antiproliferative Activities of Series 4 and 5 against Human Tumor Cell Lines.

				GI50 (μM ± SD)a
compound	R1	R		A549	KB	KBvin	DU145
4a	Cl	Me		0.043 ± 0.011	0.048 ± 0.004	0.046 ± 0.002	0.057 ± 0.011
4b	Me	Me		0.211 ± 0.038	0.204 ± 0.035	0.176 ± 0.031	0.187 ± 0.007
4c	Me	Br		0.211 ± 0.034	0.178 ± 0.028	0.169 ± 0.011	0.198 ± 0.034
compound	R1	X	Y
5a	Cl	CH2	CO	0.027 ± 0.005	0.028 ± 0.005	0.033 ± 0.005	0.031 ± 0.006
5b	Me	CH2	CO	0.024 ± 0.001	0.019 ± 0.003	0.021 ± 0.001	0.021 ± 0.004
5c	Me	CH2	CHOH	0.019 ± 0.003	0.018 ± 0.002	0.017 ± 0.001	0.018 ± 0.004
5d	Cl	CH2	O	0.199 ± 0.004	0.153 ± 0.028	0.195 ± 0.031	0.169 ± 0.021
5e	Me	CH2	O	0.189 ± 0.016	0.211 ± 0.036	0.169 ± 0.033	0.198 ± 0.033
5f	Me	CO	NH	0.0032 ± 0.0007	0.0023 ± 0.0005	0.0022 ± 0.0004	0.0019 ± 0.0004
5g	Me	CO	NMe	0.019 ± 0.002	0.017 ± 0.003	0.025 ± 0.002	0.022 ± 0.003
5h	Cl	CH2		0.233 ± 0.013	0.227 ± 0.026	0.197 ± 0.024	0.165 ± 0.035
5i	Me	CH2		0.268 ± 0.021	0.320 ± 0.056	0.216 ± 0.025	0.243 ± 0.039
5j	Cl	(CH2)2	CH2	0.191 ± 0.029	0.227 ± 0.015	0.197 ± 0.024	0.165 ± 0.035
5k	Me	(CH2)2	CH2	0.021 ± 0.002	0.019 ± 0.001	0.020 ± 0.001	0.018 ± 0.004
5l	Cl			7.57 ± 0.55	11.30 ± 0.58	5.45 ± 0.90	6.81 ± 1.34
5m	Me			16.71 ± 2.90	19.59 ± 3.33	14.76 ± 2.32	14.63 ± 1.33
paclitaxelb				0.0076 ± 0.0017	0.0064 ± 0.0014	1.21 ± 0.19	0.006 ± 0.001

^aConcentration of compound that inhibits 50% human tumor cell growth, presented as the mean ± standard deviation (SD) and performed at least in triplicate.

^bPositive control.