Table 1.

The ability of BFZ and BFX derivatives to inhibit the IN catalytic activity during 3’-processing and strand transfer reactions

Structure	No	R1	R2	Inhibitory activity, IC50, μM*
				3’-processing	strand transfer
Raltegravir				0.50 ± 0.09	0.010 ± 0.003
	1	H	-	> 1000	> 1000
	2	CH3	-	> 1000	800 ± 200
	3	Cl		> 1000	500 ± 200
	4	H	H	80 ± 20	80 ± 30
	5	CH3	H	0.4 ± 0.1	1.0 ± 0.3
	6	H	CH3	0.5 ± 0.2	0.4 ± 0.2
	7	CH3	CH3	1.0 ± 0.3	7 ± 2
	8	H	OCH3	70 ± 20	80 ± 20
	9	H		50 ± 10	80 ± 30
	10	H	Cl	20 ± 5	50 ± 10
	11	H	H	30 ± 5	40 ± 10
	12	CH3	H	2.0 ± 0.4	3.0 ± 0.6
	13	H	CH3	3.0 ± 0.6	3.0 ± 0.5
	14	OCH3	H	75 ± 12	150 ± 40
	15	H	OCH3	80 ± 30	120 ± 20
	16	H		65 ± 11	70 ± 20
	17	H	Cl	10 ± 2	45 ± 12
	18	H	-SO2-Ph	20 ± 5	15 ± 5
	19	H		10 ± 2	12 ± 3
	20	H		18 ± 6	20 ± 5
	21	H	H	400 ± 100	500 ± 120
	22	H	CH3	2.0 ± 0.4	0.3 ± 0.1
	23	H	CH2Br	6 ± 2	2.0 ± 0.5
	24	H		75 ± 15	80 ± 20
	25	H	-	0.5 ± 0.1	5 ± 2
	26	H	-	6 ± 1	5 ± 1
	27	CH3	-	100 ± 20	100 ± 30

* The average values calculated from the results of at least three repeated experiments.