. Author manuscript; available in PMC: 2016 Jun 22.

Published in final edited form as: J Med Chem. 2007 Aug 14;50(18):4340–4350. doi: 10.1021/jm061288r

Table 6.

In Vitro Activity Data of Compounds 5, 7, 8, and 16 (µM) against Various Cell Lines^a

		paclitaxel^b		1^b		5		7		8		16

cancer	cell line	GI₅₀	TGI	GI₅₀	TGI	GI₅₀	TGI	GI₅₀	TGI	GI₅₀	TGI	GI₅₀	TGI
NSCL	A549/ATCC	0.004	25.11	0.135	0.302	0.161	0.340	0.189	0.425	0.166	–	13.70	>100
	NCI-H322M	0.013	6.310	0.191	0.372	0.203	0.429	0.131	0.238	0.167	0.304	0.165	0.490
leukemia	RPMI-8226	0.002	5.012	1.738	6.918	0.475	1.780	0.638	1.890	1.270	2.760	40.10	>100
colon	COLO 205	0.003	0.316	–	–	0.156	0.315	0.618	–	0.243	–	4.520	>100
	HCC-2998	0.003	0.126	0.288	0.616	0.201	0.517	0.236	0.732	0.255	0.971	2.270	11.40
	HCT-15	0.158	15.85	0.269	0.741	0.151	0.289	0.492	1.560	0.416	1.360	0.964	17.70
	HT29	0.002	0.251	0.162	0.316	0.151	0.288	0.279	–	0.187	–	2.390	>100
	KM12	0.004	15.85	0.182	0.363	0.179	0.379	0.152	–	0.226	0.503	0.413	3.070
CNS	SNB-75	0.004	0.126	0.224	1.905	0.265	0.655	1.290	2.610	1.010	2.190	2.110	6.870
melanoma	UACC-257	0.040	25.12	1.023	2.818	1.250	0.249	1.310	2.430	1.440	2.820	> 100	>100
ovarian	SK–OV-3	0.008	15.85	0.191	0.355	0.183	0.387	0.374	1.360	0.223	0.485	2.550	20.20
renal	ACHN	0.398	12.59	1.659	3.236	1.080	2.06	1.280	2.320	1.320	2.370	26.40	69.80
prostate	PC-3	0.004	10.00	0.170	0.324	0.142	0.287	0.267	0.973	0.228	0.665	3.700	21.80
	DU-145	0.005	0.794	–	–	0.112	0.230	0.124	0.266	0.144	0.292	0.330	1.830
breast	T-47D	–	–	–	–	0.161	0.333	–	–	0.191	0.394	0.518	2.830
	HS 578T	0.003	0.100	0.162	0.479	0.212	0.695	0.162	0.444	0.427	2.130	3.030	>100

Dash (–) = no data. GI₅₀ (50% inhibition of cell growth): the concentration needed to reduce the growth of treated cells to half that of untreated (i.e., control) cells. TGI (100% (total) growth inhibition): the concentration required to completely halt the growth of treated cells.

Developmental Thrapeutics Program NCI/NIH (http://dtp.nci.nih.gov).