Table 3.

TLR signaling inhibition by C3 BSC pyrazoles with free phenols.

Cmpd	R1	R5	IC50 (μM)
			TLR9	TLR7	TLR2	TLR4	Tox.
29	p-OH	p-OH	2.65 ± 0.39	7.01 ± 1.41	9.13 ± 3.88	6.73 ± 0.66	35.0 ± 3.2
30	H	p-OH	2.61 ± 1.37	2.99 ± 0.62	6.73 ± 1.97	5.38 ± 0.64	33.3 ± 2.6
31	p-OH	H	6.80 ± 0.65	15.5 ± 1.0	7.94 ± 2.19	15.5 ± 3.1	19.9 ± 5.2
32	p-OH	m-OH	30.2 ± 0.1	n.d.	> 50	n.d.	> 50
33	p-Me	p-OH	3.97 ± 0.27	18.4 ± 0.6	23.5 ± 0.6	22.8 ± 0.7	26.3 ± 3.7
34	p-Cl	p-OH	3.79 ± 0.30	34.8 ± 0.1	11.3 ± 0.1	16.7 ± 0.5	23.6 ± 0.4
35	H	3,5-(OMe)2- 4-OH	3.23 ± 0.08	10.7 ± 0.4	5.66 ± 0.75	2.92 ± 0.22	17.7 ± 4.4
36*	p-OH	p-NH C(O)Me	1.18 ± 0.18	7.67 ± 0.21	11.0 ± 0.5	6.17 ± 0.14	9.72 ± 0.15

^*compound 36 was a 1:1 mixture of pyrazole:pyrazoline

n.d. = not determined