Design, synthesis, and biological evaluation of novel N4-substituted sulfonamides: acetamides derivatives as dihydrofolate reductase (DHFR) inhibitors

Hussein, Essam M.; Al-Rooqi, Munirah M.; Abd El-Galil, Shimaa M.; Ahmed, Saleh A.

doi:10.1186/s13065-019-0603-x

Table 2 In vitro anticancer screening of the synthesized compounds against human lung carcinoma cell line (A-549)

From: Design, synthesis, and biological evaluation of novel N⁴-substituted sulfonamides: acetamides derivatives as dihydrofolate reductase (DHFR) inhibitors

Comp. no.	Validity for sample conc.											IC₅₀ (μg mL⁻¹)^a	IC₅₀ (μM)^a
Comp. no.	500	250	125	62.50	31.25	15.60	7.80	3.90	2	1	0	IC₅₀ (μg mL⁻¹)^a	IC₅₀ (μM)^a
5a	5.19	11.84	25.06	37.15	48.91	62.87	80.96	91.43	97.02	100	100	29.90	80.06
5b	5.38	11.97	24.02	36.59	47.38	63.20	78.15	87.56	94.03	98.76	100	28.60	70.88
5c	4.31	8.65	16.37	28.74	40.96	58.71	73.04	89.21	96.28	100	100	23.20	59.87
5d	2.65	5.34	10.26	19.45	28.73	39.04	57.26	71.89	85.22	92.34	100	10.90	26.72
5e	2.94	6.71	14.09	23.87	36.29	49.85	70.63	89.24	96.31	99.72	100	15.50	34.26
5f	4.23	9.86	20.15	32.76	45.13	59.38	75.04	82.38	91.75	97.43	100	25.80	57.91
5g	2.75	6.39	10.42	18.65	28.91	40.74	56.26	70.89	83.11	88.62	100	10.90	26.11
5h	2.86	5.43	12.87	22.96	34.53	47.28	65.39	80.72	89.86	97.13	100	14.40	34.41
5i	4.73	10.59	18.42	28.96	40.67	59.23	73.18	85.21	92.74	97.35	100	23.30	62.06
5j	2.98	6.74	10.85	19.73	26.8	37.28	49.06	70.31	84.15	91.38	100	7.60	18.74
5k	8.92	16.34	24.08	35.17	49.01	72.38	89.42	98.36	100	100	100	30.50	78.31
5l	1.89	4.37	8.76	19.04	30.63	43.86	59.12	76.44	90.63	96.42	100	12.40	30.25
5m	6.72	10.86	22.38	31.49	46.75	69.42	86.03	92.34	99.71	100	100	28.90	63.61
5n	4.86	9.73	19.48	31.72	45.29	64.18	80.63	92.34	97.23	100	100	27.30	61.00
5o	2.89	6.54	15.93	24.06	36.41	52.97	68.02	79.19	91.42	98.76	100	18.30	43.63
5p	3.69	8.71	18.63	29.46	41.87	54.06	71.32	87.14	95.20	99.73	100	20.70	49.23
6a	3.65	8.29	16.34	25.87	37.06	46.92	58.43	80.71	87.53	93.14	100	13.50	36.15
6b	6.14	13.65	25.38	37.25	56.41	79.84	92.36	98.6	100	100	100	41.70	103.35
6c	3.74	7.46	15.28	27.4	41.35	56.79	68.42	82.37	91.43	97.60	100	22.40	57.81
6d	4.08	6.82	11.43	19.46	30.67	43.20	59.13	71.44	85.12	92.37	100	12.20	29.91
6e	4.62	11.29	20.47	34.13	45.29	62.37	80.94	89.76	97.02	100	100	26.80	59.24
6f	6.31	13.45	19.75	31.42	47.23	71.94	89.56	97.13	100	100	100	29.40	65.99
6g	9.56	21.87	30.64	43.19	59.46	78.28	91.40	98.76	100	100	100	49.40	118.33
6h	1.98	4.87	9.72	19.93	28.61	40.72	63.18	79.43	90.64	97.39	100	12.30	29.39
6i	7.94	11.52	24.43	36.25	49.72	71.49	89.70	97.41	100	100	100	30.90	82.30
6j	3.87	7.96	16.20	27.85	41.79	54.03	71.48	88.60	96.23	100	100	20.70	51.05
6k	7.18	12.98	23.06	33.97	47.85	63.28	78.91	90.68	97.89	100	100	29.00	74.46
6l	6.74	14.35	21.88	35.46	46.29	58.17	78.03	86.36	94.12	98.78	100	26.30	64.16
6m	4.28	9.53	18.75	31.92	40.06	47.41	73.65	90.37	98.91	100	100	14.80	32.57
6n	11.82	23.48	30.51	41.3	47.42	60.31	82.42	97.14	100	100	100	28.07	62.72
6o	31.96	49.72	73.68	90.63	97.46	100	100	100	100	100	100	248.00	591.25
6p	2.79	6.28	13.91	25.04	37.18	52.94	68.29	84.67	92.84	98.25	100	18.50	44.00
5-FU	10.28	19.45	25.39	39.48	57.21	70.82	86.19	94.36	99.25	100	100	43.9	337.48

IC₅₀ value: concentration causing 50% inhibition of cell viability
^aMean of three results obtained from three experiments

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ISSN: 2661-801X

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