Synthesis, Characterisation, and In Vitro Anticancer Activity of Curcumin Analogues Bearing Pyrazole/Pyrimidine Ring Targeting EGFR Tyrosine Kinase

Table 3

NCI in vitro testing results of compounds of the compounds 8, 10, and 13 at five-dose level in µM.

S. no.	Panel/cell line	8 (NSC 757926)			10 (NSC 757929)			13 (NSC 763375)
		GI50	TGI	LC50	GI50	TGI	LC50	GI50	TGI	LC50
(1)	Leukemia
	CCRF-CEM	0.232	>100	>100	0.127	>100	>100	0.543	NT	>100
	HL-60(TB)	0.237	0.806	>100	0.0884	NT	>100	2.18	6.17	>100
	MOLT-4	0.364	NT	>100	0.347	>100	>100	1.01	5.19	>100
	RPMI-8226	0.336	NT	>100	0.275	NT	>100	1.29	4.18	>100
	SR	0.004	>100	>100	0.0353	>100	>100	0.72	3.58	>100
(2)	Non-small cell lung cancer
	A549/ATCC	0.445	3.63	56.3	0.403	1.91	>100	2.22	6.04	76.4
	EKVX	0.771	5.51	>100	0.702	2.38	NT	2.22	6.83	>100
	HOP-62	0.497	1.63	4.21	0.441	1.62	4.23	1.96	4.28	NT
	HOP-92	0.538	3.39	>100	0.35	3.32	>100	1.26	5.19	>100
	NCI-H226	0.389	2.1	12.9	0.382	1.83	7.68	1.83	4.34	12
	NCI-H23	0.275	1.25	>100	0.113	1.61	>100	1.8	4.24	NT
	NCI-H322M	0.571	2.8	85.8	0.615	2.49	NT	2.22	5.39	>100
	NCI-H460	0.306	NT	>100	0.274	NT	>100	2.05	5.20	>100
	NCI-H522	0.13	0.616	NT	0.286	7.59	NT	1.24	2.79	6.31
(3)	Colon cancer
	COLO 205	2.05	3.62	6.38	1.86	3.34	5.97	1.8	3.24	5.85
	HCC-2998	0.64	5.8	>100	0.591	2.71	>100	1.75	3.19	5.79
	HCT-116	0.323	NT	NT	0.269	1.14	NT	1.1	2.39	5.18
	HCT-15	0.335	1.66	NT	0.167	1.52	NT	2.82	10.3	>100
	HT29	0.696	2.8	9.94	0.463	3.19	>100	3.14	0.948	4.21
	KM12	0.298	1.25	NT	0.0092	1.19	NT	1.63	3.32	6.79
	SW-620	0.441	NT	>100	0.0079	NT	>100	1.65	3.68	NT
(4)	CNS cancer
	SF-268	0.571	NT	NT	0.256	NT	NT	2.11	15.6	>100
	SF-295	0.546	NT	>100	0.538	NT	NT	1.93	4.54	>100
	SF-539	0.354	1.5	NT	0.0604	1.53	NT	2.05	5.73	>100
	SNB-19	0.634	2.01	NT	0.572	2.12	NT	1.81	7.95	>100
	SNB-75	0.416	1.82	NT	0.0099	1.87	NT	1.26	3.34	8.84
	U251	0.471	1.59	NT	0.428	1.70	NT	1.79	5.69	6.63
(5)	Melanoma
	LOX IMVI	0.284	1.49	NT	0.0626	1.56	NT	1.27	2.59	NT
	MALME-3M	0.563	1.98	NT	0.525	2.17	NT	2.71	6.76	>100
	M14	0.372	1.41	NT	0.155	1.48	NT	1.65	3.44	NT
	MDA-MB-435	0.0448	0.383	NT	0.0175	0.00815	>100	1.71	NT	>100
	SK-MEL-2	0.366	1.82	NT	0.266	2.03	>100	1.98	4.1	NT
	SK-MEL-28	0.509	2.47	8.61	0.176	2.72	9.05	1.85	4.53	26
	SK-MEL-5	0.317	1.29	3.67	0.171	1.30	3.69	1.49	2.89	5.59
	UACC-257	1.54	5.47	31.9	1.14	4.29	53.3	1.53	3.5	8
	UACC-62	0.413	1.65	4.89	0.371	1.64	NT	1.49	3.23	NT
(6)	Ovarian cancer
	IGROV1	0.454	2.62	>100	0.483	NT	>100	2.95	7.08	>100
	OVCAR-3	0.412	1.72	>100	0.242	1.16	>100	2.65	8.62	63.5
	OVCAR-4	0.481	3.32	>100	0.530	6.76	>100	1.71	11.5	71.1
	OVCAR-5	1.51	6.85	>100	1.27	4.51	>100	2.03	4.33	9.22
	OVCAR-8	0.563	2.35	9.71	0.479	3.78	>100	2.19	7.24	>100
	NCI/ADR-RES	0.338	4.01	>100	0.0874	3.85	>100	2.88	18.8	>100
	SK-OV-3	0.419	1.6	7.28	0.358	1.35	3.88	2.6	8.23	>100
(7)	Renal cancer
	786-0	0.549	1.76	4.61	0.688	2.03	4.99	1.7	4	NT
	A498	0.575	1.98	4.63	0.697	2	4.65	1.51	3.26	7.04
	ACHN	0.412	2.11	>100	0.131	1.69	NT	2.54	7.88	>100
	CAKI-1	0.341	5.49	>100	0.282	3.24	>100	2.23	6.46	>100
	RXF 393	0.227	0.653	2.72	0.263	0.878	3.60	1.5	3.2	NT
	SN 12C	0.339	1.88	NT	0.313	2.20	>100	2.74	>100	>100
	TK-10	0.424	2	7.15	0.446	1.76	5.19	3.39	9.54	5.34
	UO-31	0.362	1.74	5.93	0.258	1.65	4.73	2.09	7.57	>100
(8)	Prostate cancer
	PC-3	0.349	5.78	>100	0.331	12.7	>100	1.48	5.57	>100
	DU-145	0.419	1.44	NT	0.389	1.51	NT	2.4	6.31	88
(9)	Breast cancer
	MCF7	0.317	1.37	4.86	0.162	1.6	6.57	1.81	6.33	38.8
	MDA-MB-231/ATCC	0.473	4.71	>100	0.404	4.83	>100	1.45	4.08	>100
	HS 578T	0.295	>100	>100	0.0779	>100	>100	0.524	2.99	>100
	BT-549	0.693	16.8	>100	0.631	22.8	>100	1.3	3.52	NT
	T-47D	0.79	2.94	NT	0.793	2.93	9.79	2.83	9.55	>100
	MDA-MB-468	0.248	0.825	63.1	0.276	0.969	>100	NT	NT	NT

NT: not tested.