Table 1.

Cytotoxicity, Antiviral and Anti-Integrase Activities of Derivatives 5–8

			Anti-IN Activity					Antiviral Activity
Cpd	R	X	IC50a					CC50d	EC50e	SI f
			ST			3′-P
			Mg2+b	Mg2+c	Mn2+c	Mg2+c	Mn2+c
5	H	C2H5	77 ± 13	39	80	28	>333	>200	>50	-
6	H	H	9.1 ±1.2	2.9	0.43	22	>4.1	>200	36.3	5.5
7	Bzg	C2H5	0.38 ± 0.01	0.29	0.25	21	40	191	20	9.6
8	Bzg	H	0.016 ± 0.004	0.017	0.012	0.44	0.20	>200	4.29h	>47
2i					1.83		7.8	nrj	nr	-
3i					6.5		82	>25	61k	-
4i					0.2		1.8	81	17	4.8

^aInhibitory concentration 50% (μM) determined from dose-response curves.

^bExperiments performed in triplicate using the BioVeris assay (ST assay in the presence of MgCl₂).

^cExperiments performed on gels in the presence of MnCl₂ or MgCl₂ (see Figure 3).

^dCytotoxic concentration 50% (μM).

^eEffective concentration 50% (μM).

^fSelectivity index = CC₅₀/EC₅₀.

^gBz = CH₂-4-F-Ph.

^hFor this compound EC₉₀ = 40 μM was determined.

ⁱLiterature data see references 11–13.

^jnr: not reported.

^kPercentage of inhibition obtained at a concentration of 25 μM.