Table 4.

In vitro integrase inhibition activities of the 7-aroyl-styrylquinolines derivatives.

	3’-Processing IC50 (μM)	Strand Transfer IC50 (μM)	References
59a, R = H	82.0	Untested	30
59b, R = Ph	50.0a	Untested	33
59c, R = 1-Naphthyl	92.0	Untested	33
59da, R = CH3	0.2	0.2	34
59e, R = C8H17	>100.0 b	Untested	33
59f, R = PhCH2CH2	>100.0 a	Untested	33
59g, R = 4-NO2Ph	100.0	>100.0	33
59h, R = 2-NO2Ph	>100.0	70.0	33
59i, R = 3,4-F2Ph-	24.0	>100.0	33
59j, R = 4-pyridyl	>100.0 a	Untested	33
59k, R = 3-pyridyl	>100.0	>100.0	33
59l, R = 2-OH-Ph	>100.0	>100.0	33
5m, R = 4-OH-Ph	65.0	>100.0	33
59n, R = 4-(HO2C)Ph	0.2	Untested	33
59o, R = 3-(HO2C)Ph	0.2	Untested	33
59p, R = 2-(HO2C)Ph	0.3	Untested	33

^a 1,3,4-trihydroxyphenyl instead of the 3,4-dihydroxyphenyl ancillary ring. ^b Overall binding assay.