Table 1.

In vitro antiproliferative activities of 2–(4-((-pyrimidin-2-yl)amino)benzoyl) hydrazine-1-carboxamide derivatives (Series A) on two selected cancer cell lines.^a

Compounds	R1	R2	X	IC50[μM]
				HepG2	A549
6a	4-Pyridyl	n-Butyl	O	5.32 ± 0.07	21.69 ± 1.33
6b	4-Pyridyl	t- Butyl	O	5.39 ± 0.11	18.09 ± 1.25
6c	4-Pyridyl	Cyclohexyl	O	2.17 ± 0.08	8.39 ± 0.92
6d	4-Pyridyl	Cyclopentyl	O	2.71 ± 0.13	16.26 ± 1.21
6e	4-Pyridyl	p-Tolyl	O	1.28 ± 0.09	11.27 ± 1.05
6f	4-Pyridyl	2,4-difluorophenyl	O	8.10 ± 0.12	26.38 ± 1.42
6g	4-Pyridyl	3-chloro-4-methylphenyl	O	>40	>40
6h	4-Pyridyl	Phenethyl	O	3.89 ± 0.04	13.11 ± 1.11
6i	3-Pyridyl	n-Butyl	O	>40	38.93 ± 1.59
6j	3-Pyridyl	Cyclopentyl	O	5.73 ± 0.26	17.09 ± 1.23
6k	3-Pyridyl	p-Tolyl	O	>40	8.385 ± 0.92
6l	3-Pyridyl	Phenethyl	O	5.48 ± 0.21	23.71 ± 1.37
6m	2-Pryidyl	n- Butyl	O	>40	>40
6n	2-Pryidyl	t-Butyl	O	15.71 ± 0.11	>40
6o	2-Pryidyl	Cyclopentyl	O	>40	>40
6p	2-Pryidyl	m-Tolyl	O	23.31 ± 0.07	>40
6q	2-Pryidyl	3,5-dimethylphenyl	O	20.32 ± 0.14	>40
6r	4-Chlorophenyl	t- Butyl	O	4.48 ± 0.09	19.49 ± 1.29
6s	4-Chlorophenyl	Ethyl	O	20.34 ± 0.34	>40
6t	4-Chlorophenyl	Cyclohexyl	O	13.08 ± 0.46	>40
6A	4-Pyridyl	Phenyl	S	5.13 ± 0.14	5.09 ± 0.70
6B	4-Pyridyl	Benzyl	S	0.61 ± 0.07	15.95 ± 1.20
6C	3-Pyridyl	Benzyl	S	1.47 ± 0.42	17.57 ± 1.24
6D	2-Pryidyl	Phenyl	S	6.74 ± 0.05	38.51 ± 1.58
6E	2-Pryidyl	Benzyl	S	4.59 ± 0.11	>40
6F	Phenyl	Cyclohexyl	S	>40	30.79 ± 1.48
6G	Phenyl	Phenyl	S	>40	20.68 ± 1.31
6H	Phenyl	Benzyl	S	>40	22.27 ± 1.34
6I	4-Chlorophenyl	Phenyl	S	17.24 ± 0.07	28.32 ± 1.45
6J	4-Chlorophenyl	Benzyl	S	1.29 ± 0.09	12.76 ± 1.10
Sorafenib				16.89 ± 1.22	>40

^aData are means ± SD of triplicate experiments.