Table 1.

Scaffold screening: inhibition of HIV-1 integrase catalytic activities and the cytotoxicityby salicylic acid derivatives with various substitution pattern.

Compd	R1	R2	IC50 (μM)		CC50 (μM) H630 cells
			3′-Processing	Strand transfer
3a		OH	> 100	> 100	> 40
3b		OH	> 100	> 100	> 40
3c		OH	> 100	140±46	> 40
3d		OH	> 100	> 100	> 40
3e		OH	> 100	> 100	> 40
3f		OH	> 100	> 100	> 40
3g		OH	> 100	> 100	> 40
3h		OH	> 100	> 100	> 40
3i		OH	> 100	> 100	> 40
3j		OH	> 100	186±15	> 40
4a		NHOH	> 100	> 100	NDa
4b		NHOH	> 100	100	ND
4c		NHOH	> 100	85±7	ND
4d		NHOH	> 100	97±6	ND
5a	3-OH		100	35±25	> 40
5b	3-OBn		> 333	111	> 40

^aND: not determined.