Table 1.

The Anti-Cancer Activities of Imidazole Derivatives Using Several Cancer Cell Lines

Chemical Structure	Cell Line	Activity	Mechanism	Reference
	Kidney cancer cells (HEK 293)	LC50 (µM)	Topoisomerase IIR catalytic inhibitors. The apoptotic effect in the G1/S phase.	[9]
	Breast cancer cells (MCF7)	15 at both cell lines
		IC50 (µM)	Induce apoptosis. Bind with DNA through intercalation.	[10]
	Cervix cancer cells (HeLa)	2.88 ± 0.15
	Breast cancer cells (MCF-7)	0.75 ± 0.07
	Lung cancer cells (A549)	4.37 ± 0.07
	Liver cancer cells (HepG2)	2.91 ± 0.11
		IC50 (µM)	Focal Adhesion Kinase (FAK) inhibition. Arrest cells in the G2/M phase of the cell cycle. Retard cell growth	[12]
	Brain (U87-MG)	0.37±0.04
	Colon (HCT-116)	0.31±0.18
	Breast (MDA-MB)-231	1.08±0.45
	Prostate (PC-3)	1.27±0.28
		IC50 (µM)	Decreases angiogenesis in the peritoneum of EAT bearing mice.	[14]
	Cervical (HeLa)	25.3
		GI50 (µM)	Cyclin-dependent kinase 6 (CDK6) inhibition and induce cancer cell apoptosis.	[15]
	Colon (HCT-116)	3.0
	Breast (MCF-7)	40
		IC50 (µM)	Selective inhibitor for the HUVECs. Activation of p38 signaling pathway.	[16]
	Human umbilical vein endothelial cells (HUVECs)	0.4
	Smooth muscle cells (SMCs)	5.5
		IC50 (µM)	Exhibited excellent inhibitory activity on tumor growth in vivo	[17]
	Human myeloid leukemia cells (HL-60)	0.2
	Human myeloid leukemia cells (K562)	1
	Human myeloid leukemia cells (K562R) (multidrug-resistant cells)	0.9
	Human prostate carcinoma cells (PC-3)	3.1
	Human breast carcinoma cells (MCF-7)	10.6
	Human esophageal carcinoma cells (ECA-109)	3.8
	Human hepatocarcinoma cells (BEL-7402)	1.2
	Human non-small lung cancer cells (A549)	1.3
		IC50 (µM)	Inhibit tubulin polymerization and arrest cell cycle at G2/M phase	[21]
	MCF-7	9.450±0.292
	H1299	7.652±0.215
	HeLa	6.862±0.144
	B16-F10	4.912±0.088
	HUVEC	>50
		IC50 (µM)	Arrest cell cycle at G1 phase and induce apoptosis	[22]
	HeLa	82.83±1.37
		GI50 (µM)	ND Possibly due to dimerized estrogen receptor	[18]
	Cervical (HeLa)	0.36
	Breast (MDA-MB-231)	0.30
	Renal cancer (ACHN)	0.38
		IC50 (µM)	c-MYC G-quadruplex DNA stabilizers	[19]
	Nasopharyngeal carcinoma (CNE-1)	1.1± 0.1
		IC50 (µM)	Aurora kinase inhibition	[20]
	breast cancer (MDA-MB-231)	0.38±0.08
	prostate cancer (PC3)	1.09 ±0.24
	neuroblastoma (SH-SY5Y)	0.77±0.12
		IC50 (µM)	Inhibit BRAFV600E kinase	[23]
	NCI 60	2.4
	LOX IMVI	1.75
	MALME-3M	1.69
	M14	1.76
	MDA-MB-435	1.97
	SK-MEL-2	2.21
	SK-MEL-28	2.13
	SK-MEL-5	1.60
	UACC-257	2.08
	UACC-62	1.85
		IC50 (µM)	Inhibit GSK-3β	[24]
	Caco-2	4.67 ± 0.11
	HCT-116	16.78 ± 0.59
	HeLa	6.87 ± 0.32
	MCF-7	0.38 ± 0.04
		IC50 (µM)	Anti-proliferative	[11]
	Melanoma (human A375)	16.1±0.5
	Melanoma (mouse B16)	31.6±1.1
	Cervical (HeLa)	IC50 (µM) >25 for all the cell lines	ND	[13]
	Colon (LS180)
	Breast (MCF-7)
	Jurkat cells
		IC50 (µΜ)	ND	[25]
	A549	0.93 ± 0.34
	PC3	0.83 ± 0.27
	PANC	0.063 ± 0.09
	ASPC-1	0.062 ± 0.013

Note: Values are means of three experiments.

Abbreviation: LC₅₀, The concentration required to kill half the cells in the cell culture; IC₅₀, Compound concentration required to inhibit tumor cell proliferation by 50%; GI₅₀, The concentration of drug causing 50% inhibition of cell growth; ND, Not determined.