Table 1.

In vitro antiproliferative study (IC₅₀ values µM) of the final target compounds 4a-e and 5a-j against four cancer cell lines and WI38 normal cell line, in comparison with DOX and Afatinib.

Comp. No.	R	R1	In vitro Cytotoxicity IC50 (µM)a
			MCF7	HCT-116	PC3	A549	WI38
4a	CH3	Cl	8.74 ± 0.42	13.47 ± 0.57	12.71 ± 0.49	2.026 ± 0.09	75.71 ± 4.3
4b	CH3	N(CH3)2	26.43 ± 1.27	31.02 ± 1.32	59.25 ± 2.28	42.54 ± 1.91	60.35 ± 3.7
4c	C2H5	N(CH3)2	79.98 ± 3.83	56.20 ± 2.39	55.04 ± 2.12	48.53 ± 2.18	55.30 ± 3.3
4d	CH3	OH	10.08 ± 0.48	2.68 ± 0.11	2.371 ± 0.09	23.20 ± 1.04	33.26 ± 2.3
4e	C2H5	OH	35.55 ± 1.51	49.45 ± 2.1	22.2 ± 0.86	20.62 ± 0.93	47.53 ± 2.9
5a	CH3	H	1.673 ± 0.07	5.602 ± 0.24	12.33 ± 0.48	5.827 ± 0.26	49.62 ± 3.0
5b	C2H5	H	6.033 ± 0.27	2.991 ± 0.13	9.09 ± 0.35	1.904 ± 0.09	65.6 ± 2.7
5c	CH3	Cl	2.904 ± 0.11	2.575 ± 0.13	2.56 ± 0.13	8.029 ± 0.36	100
5d	C2H5	Cl	23.58 ± 0.92	21.74 ± 0.88	27.22 ± 1.05	47.67 ± 2.14	100
5e	CH3	NO2	10.85 ± 0.42	20.74 ± 0.88	19.15 ± 0.74	71.46 ± 3.21	67.22 ± 3.9
5f	C2H5	NO2	56.79 ± 2.21	62.74 ± 2.67	11.33 ± 0.44	21.73 ± 0.98	57.46 ± 2.4
5 g	CH3	OCH3	6.674 ± 0.28	1.154 ± 0.05	3.302 ± 0.13	29.36 ± 1.32	72.93 ± 4.2
5 h	C2H5	OCH3	38.95 ± 1.72	19.74 ± 0.84	15.51 ± 0.6	24.05 ± 1.08	83.47 ± 4.6
5i	CH3	CH3	21.43 ± 0.91	7.75 ± 0.33	9.71 ± 0.37	5.129 ± 0.23	66.27 ± 3.7
5j	C2H5	CH3	18.99 ± 0.84	21.31 ± 0.91	5.47 ± 0.21	11.91 ± 0.53	100
Afatinib	–	–	5.10 ± 0.31	10.01 ± 0.47	7.98 ± 0.37	8.09 ± 0.69	49.50 ± 2.5
DOX	–	–	4.50 ± 0.2	5.23 ± 0.3	4.17 ± 0.2	5.57 ± 0.4	6.72 ± 0.5

^aIC₅₀ value is the concentration of compound that inhibits 50% of the cancer cell growth after 48 h of drug exposure as obtained from the MTT assay. Each value was shown as mean ± SD of three experiments. Bolded values represent the most potent antiproliferative derivatives.