. Author manuscript; available in PMC: 2016 Jan 27.

Published in final edited form as: Eur J Med Chem. 2014 Dec 11;90:775–787. doi: 10.1016/j.ejmech.2014.11.062

Table 1.

In vitro cytotoxic activities of hydroxy derivatives of 2-arylnaphthyridin-4-ones (6a–e, 6g–i, 7a–i).


						IC₅₀^a,^b (μM)
Cmpd	R₅	R₆	R₇	R₃′	X	HL-60^c	Hep3B^c	NCI-H460^c	Detroit551^c

6a	CH₃	H	H	OCH₃	-	0.03	0.13	0.18	>5.0
7a	CH₃	H	H	OH	-	0.03	0.17	0.20	>50
6b	H	CH₃	H	OCH₃	-	0.06	0.12	0.14	>2.5
7b	H	CH₃	H	OH	-	0.08	0.44	0.45	>2.5
6c	CH₃	H	CH₃	OCH₃	-	0.33	0.73	0.75	>50
7c	CH₃	H	CH₃	OH	-	0.29	0.68	1.30	>100
6d	H	Cl	H	OCH₃	-	0.03	0.10	0.10	>50
7d	H	Cl	H	OH	-	0.11	0.34	0.20	>100
6e	H	F	H	OCH₃	-	0.07	0.20	0.24	>5.0
7e	H	F	H	OH	-	0.14	0.38	0.70	>100
7f	OH	H	H	F	-	0.82	1.82	2.48	>100
6g	H	OCH₃	H	F	-	0.02	0.02	0.05	>10
7g	H	OH	H	F	-	0.08	0.16	0.86	>100
6h	H	OCH₃	H	-	–CH=CH-	0.04	0.05	0.85	>25
7h	H	OH	H	-	–CH=CH-	0.48	0.46	1.34	>100
6i	H	OCH₃	H	-	S	0.04	0.09	0.16	>10
7i	H	OH	H	-	S	0.57	1.07	0.39	10
Taxol	-	-	-	-	-	0.002	0.50	0.005	NT^d

Data was presented as IC₅₀ (μM, the concentration of 50% proliferation-inhibitory effect).

Human tumor cells were treated with different concentrations of samples for 48 h.

HL-60, human leukemia cell line; Hep3B, human hepatoma cell line; NCI-H460, non-small cell lung cancer cell line; Detroit 551, human skin fibroblast cell line.

NT = not tested.