Table 2.

Inhibitory activity of 5–8 against HTCL panel

	R3	R4	GI50 ± SD (μM)b
			A549	KB	KBVIN	DU145
3a	NO2	Cl	2.20±0.20	1.78±0.11	1.86±0.30	1.55±0.24
5a	NO2	Me	4.42±0.44	2.92±0.25	4.19±0.97	3.35±0.55
5b	NO2	OMe	3.27±0.69	3.31±0.46	2.83±0.71	2.70±0.25
5c	NO2	NHMe	4.50±0.35	4.53±0.70	9.63±1.14	4.45±0.85
6a	COOMe	Cl	0.23±0.01	0.26±0.04	0.20±0.03	0.21±0.04
6b	COOMe	OMe	3.15±0.75	4.01±0.75	4.02±0.57	2.45±0.49
6c	COOMe	NHMe	3.43±0.30	1.36±0.34	0.92±0.09	1.67±0.13
7a	CN	Cl	20.4±2.51	22.1±1.94	18.1±3.73	20.4±4.59
7b	COOEt	Cl	1.81±0.12	1.80±0.10	1.43±0.18	1.43±0.09
7c	COOH	Cl	NA	NA	NA	NA
7d	COOPr-i	Cl	22.0±1.64	14.5±0.40	17.3±1.58	17.8±0.34
7e	CONHMe	Cl	NA	NA	NA	NA
7f	CH2OH	Cl	3.25±0.27	2.26±0.10	2.12±0.16	1.96±0.11
7g	CH2OMe	Cl	0.30±0.03	0.33±0.07	0.20±0.01	0.25±0.01
8c	COOMe	CF3	0.35±0.05	0.41±0.09	0.19±0.01	0.25±0.04
8d	COOH	CF3	NA	NA	NA	NA
8e	COOEt	CF3	1.46±0.13	1.52±0.10	1.30±0.15	1.30±0.13
8f	COOPr-i	CF3	NA	NA	NA	NA
8g	CONHMe	CF3	NA	NA	NA	NA
8h	CH2OH	CF3	2.13±0.09	1.92±0.28	1.75±0.11	1.71±0.08
8i	CH2OMe	CF3	1.20±0.02	1.64±0.04	1.43±0.20	1.29±0.11
8j	CN	CF3	7.21±1.20	15.3±2.33	7.91±1.56	10.7±2.49
8k		CF3	NA	NA	NA	NA
8l		CF3	1.82±0.50	1.47±0.34	1.26±0.09	1.16±0.05
Paclitaxelc			8.18±1.01 nM	7.77±0.84 nM	1803±302 nM	6.50±0.43 nM

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

^bNot active; test compound (20 μg/mL) did not reach 50% inhibition.

^cPositive control.