Structure–activity relationship guided design, synthesis and biological evaluation of novel diaryl urea derivatives as antiproliferative agents

Table 1 In vitro antiproliferative activities (IC₅₀) of synthesized compounds (4a-b, 6a-g, 8a-b and 9a-f) against HT-29 and A549 cells.^a


Compound	R₁	R₂	n	IC₅₀ (µM)^a,b ± SEM^c
Compound	R₁	R₂	n	HT-29	A549
4a	H	–	–	120.7 ± 1.95	61.92 ± 1.86
4b	4-Cl	–	–	176.8 ± 3.14	71.48 ± 3.10
6a	4-Cl	5-nitrobenzo[b] thiophene	0	15.28 ± 2.62	2.566 ± 2.23
6b	4-Cl	4-methylphenyl	0	55.66 ± 2.27	17.05 ± 2.26
6c	4-Cl	phenyl	0	95.66 ± 2.02	161.4 ± 1.51
6d	4-Cl	phenyl	1	58.50 ± 3.84	30.66 ± 2.09
6e	H	4-methylphenyl	0	142.6 ± 5.54	125.3 ± 2.47
6f	H	phenyl	0	22.89 ± 2.19	2.250 ± 1.60
6 g	H	phenyl	1	131.3 ± 1.66	170.6 ± 2.61
8a	H			1527	81.91 ± 1.98
8b	4-Cl	–	–	9771 ± 3,13	152.4 ± 2.83
9a	4-Cl	5-nitrobenzo[b] thiophene	0	114.4 ± 2.62	99.67 ± 2.23
9b	4-Cl	3-methyl-5-nitrobenzene[b] thiophene	0	118.2 ± 3.39	176.5 ± 2.03
9c	4-Cl	4-methylphenyl	0	138.3 ± 3.86	93.88 ± 2.24
9d	4-Cl	phenyl	0	111.5 ± 2.79	361.9 ± 1.54
9e	4-Cl	phenyl	1	113.3 ± 6.34	105.8 ± 1.74
9f	H	phenyl	0	143.3 ± 3.59	66.33 ± 2.11
sorafenib				14.01 ± 1.59	2.913 ± 2.57

^aCells were treated with different concentrations of compounds for 24 h. Cell viability was measured by MTT assay as described in the Experimental Section. ^bIC₅₀ values are indicated as mean of at least three independent experiments [12]. ^cstandard error of the mean (SEM)

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