Table 1.

Structures and activity of target compounds 10a–e and 11a–e.

Compd.	X	R2	IC50a (μM)
			A549	HepG2	MCF-7	LogD7.4e
10a	O	—H	NAc	35.23 ± 1.53	33.42 ± 0.97	4.05
10b	O	—CH3	28.22 ± 1.34	33.25 ± 1.46	34.76 ± 1.01	4.25
10c	S	—CH3	28.35 ± 0.56	29.22 ± 1.43	26.12 ± 1.33	5.55
10d	S	—CH2CH3	34.23 ± 0.31	36.20 ± 1.78	NDd	6.01
10e	N	—H	2.41 ± 0.32	0.59 ± 0.02	1.21 ± 0.19	3.99
11a	O	—H	26.23 ± 1.23	29.69 ± 1.86	NDd	4.15
11b	O	—CH3	28.22 ± 1.34	30.21 ± 1.16	35.16 ± 081	4.35
11c	S	—CH3	29.33 ± 0.36	27.42 ± 1.03	28.12 ± 1.13	5.65
11d	S	—CH2CH3	35.28 ± 0.42	35.23 ± 1.08	NDd	6.09
11e	N	—H	8.41 ± 0.76	9.18 ± 1.05	9.31 ± 1.76	4.09
Afatinibb	–	–	6.34 ± 0.01	1.16 ± 0.06	1.09 ± 0.01	2.34

^aValues are presented as the mean ± SD in two independent experiments.

^bUsed as a positive control.

^cNA: not active.

^dND: Not determined.

^eThe result is predicted by https://chemaxon.com/#/calculation.