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 3 In vitro anticancer screening of the synthesized compounds against human breast carcinoma cell line (MCF-7)

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	7.34	14.03	29.47	41.58	54.29	71.43	87.50	96.75	100	100	100	41.80	111.92
5b	7.13	13.42	30.96	42.37	56.29	68.41	83.77	91.40	98.32	100	100	45.40	112.52
5c	5.28	11.32	20.79	32.65	48.51	70.38	86.42	94.03	99.71	100	100	30.10	77.68
5d	3.46	7.28	15.09	27.41	36.27	45.62	63.18	80.94	93.46	99.53	100	13.70	33.59
5e	4.02	9.56	18.48	29.67	40.82	54.61	73.28	91.42	98.70	100	100	20.80	45.98
5f	6.17	14.38	27.56	39.4	53.29	68.43	81.70	93.68	99.85	100	100	38.70	86.86
5g	3.86	8.24	15.37	24.16	32.95	41.68	49.80	67.48	85.26	93.84	100	7.76	18.59
5h	3.94	7.81	16.23	31.42	39.79	48.20	67.41	82.76	91.30	98.72	100	14.90	35.61
5i	6.28	13.47	25.13	36.78	48.50	67.41	81.67	89.43	98.16	100	100	30.00	79.91
5j	4.17	9.82	18.78	27.05	35.23	46.19	54.82	69.46	87.34	94.29	100	12.10	29.84
5k	13.49	21.86	32.75	46.23	57.18	76.94	88.60	97.41	100	100	100	51.70	132.74
5l	2.73	6.46	11.38	24.95	34.89	42.67	51.53	65.76	83.20	91.42	100	9.140	22.30
5m	9.85	18.2	30.67	42.96	51.78	68.92	84.68	95.41	99.62	100	100	37.50	82.54
5n	7.63	15.26	27.39	38.04	46.15	58.20	71.36	88.42	96.28	100	100	26.20	58.55
5o	3.46	9.82	20.31	29.57	43.60	56.89	70.42	83.97	92.40	97.36	100	23.60	56.26
5p	4.98	11.75	21.42	36.75	50.38	69.41	85.26	93.02	99.76	100	100	32.10	76.35
6a	4.94	10.73	23.4	32.79	45.17	56.24	71.38	85.02	92.47	98.25	100	24.40	65.33
6b	8.71	20.42	37.53	49.81	62.97	85.46	93.04	99.32	100	100	100	62.00	153.66
6c	5.31	9.14	19.56	32.71	49.82	70.38	81.6	92.88	98.76	100	100	31.10	80.26
6d	6.79	13.4	19.85	27.93	36.7	48.61	63.87	76.45	88.29	96.36	100	14.90	36.53
6e	7.46	19.53	28.65	40.37	52.91	69.42	82.36	91.73	98.6	100	100	38.50	85.11
6f	9.56	17.28	28.67	36.7	50.98	67.39	82.15	93.69	98.72	100	100	33.40	74.97
6g	15.68	27.83	38.17	52.46	69.9	83.51	92.78	99.52	100	100	100	73.30	175.58
6h	2.37	7.54	15.18	23.65	34.89	45.13	60.97	75.86	87.41	95.64	100	13.20	31.54
6i	11.76	21.49	34.85	43.96	58.28	77.39	91.47	97.92	100	100	100	49.30	131.31
6j	5.92	11.48	23.69	34.73	47.21	68.46	80.93	92.64	98.23	100	100	29.14	71.87
6k	12.41	20.53	30.78	39.62	56.34	71.48	86.24	98.4	100	100	100	43.00	110.41
6l	10.32	19.67	32.94	41.78	51.85	65.04	79.12	90.65	97.54	100	100	36.90	90.02
6m	7.64	16.29	24.31	35.17	45.04	56.28	69.46	82.78	94.13	99.2	100	24.30	53.48
6n	19.47	31.85	40.91	49.76	58.49	71.32	86.95	97.81	100	100	100	61.60	137.65
6o	37.04	52.31	76.45	91.32	98.74	100	100	100	100	100	100	287.00	684.23
6p	3.45	9.74	20.37	31.96	46.29	70.34	85.21	93.18	99.4	100	100	28.70	68.26
5-FU	9.18	17.84	28.01	35.39	47.13	60.35	71.82	86.97	95.23	98.12	100	27.80	213.71

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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