Table 2.

Summary of biological activities of compounds 4–16.^a

Cmpd	FP assay		RNA cross-linking assay		Reticulocyte lysate assay	35S-Met incorporation assay
	Inhibition (%)b	Kd (μM)	Inhibition (%)b	IC50 (μM)	IC50 (μM)	IC50 (HeLa)	IC50 (MCF-7)
m7GTP	97.3 ± 2.4c	0.37 ± 0.03	92.8 ± 1.6c	0.72 ± 0.14	8.6 ± 1.1	Inactive	Inactive
m7GMP	86.3 ± 5.0	3.9 ± 0.5	97.5 ± 0.8	1.7 ± 0.1	46.9 ± 3.4	Inactive	Inactive
4a	14.4 ± 3.2	n.d.d	Inactive	n.d.	n.d.	n.d.	n.d.
4b	9.1 ± 5.5	n.d.	Inactive	n.d.	n.d.	n.d.	n.d.
4c	15.2 ± 4.7	n.d.	Inactive	n.d.	n.d.	n.d.	n.d.
4d	2.0 ± 6.3	n.d.	Inactive	n.d.	n.d.	n.d.	n.d.
4e	Inactive	n.d.	Inactive	n.d.	n.d.	n.d.	n.d.
4f	13.2 ± 4.2	n.d.	Inactive	n.d.	n.d.	n.d.	n.d.
4g	3.9 ± 5.2	n.d.	Inactive	n.d.	n.d.	n.d.	n.d.
4h	1.8 ± 7.7	n.d.	6.5 ± 7.1	n.d.	n.d.	n.d.	n.d.
4i	Inactive	n.d.	Inactive	n.d.	n.d.	n.d.	n.d.
7a	89.0 ± 1.7	56.5 ± 6.9	42.9 ± 4.8	12.6 ± 0.5	65.9 ± 13.6	Inactive	Inactive
7b	49.4 ± 6.3	133 ± 28	48.6 ± 1.3	18.7 ± 5.0	165 ± 32	Inactive	Inactive
7c	Inactive	n.d.	22.2 ± 1.8	n.d.	n.d.	n.d.	n.d.
11a	9.7 ± 2.9	n.d.	25.8 ± 2.9	n.d.	n.d.	n.d.	n.d.
11b	30.2 ± 2.8	n.d.	15.3 ± 4.8	n.d.	n.d.	n.d.	n.d.
12a	13.6 ± 2.2	n.d.	10.2 ± 3.3	n.d.	n.d.	n.d.	n.d.
12b	25.8 ± 5.9	n.d.	Inactive	n.d.	n.d.	n.d.	n.d.
12c	8.5 ± 2.8	n.d.	Inactive	n.d.	n.d.	n.d.	n.d.
13	Inactive	n.d.	Inactive	n.d.	n.d.	n.d.	n.d.
14	68.1 ± 0.8	57.8 ± 13.5	47.5 ± 6.7	38.6 ± 10.6	65.1 ± 12.5	35.2 ± 4.0	37.7 ± 10.4
15	Inactive	n.d.	3.5 ± 3.2	n.d.	n.d.	n.d.	n.d.
16	Inactive	n.d.	33.8 ± 8.1	n.d.	n.d.	n.d.	n.d.

^aAll experiments were carried out on three independent occasions.

^bAt 100 μM concentration unless otherwise indicated.

^cAt 10 μM concentration.

^dNot determined.