Table 1.

Cytotoxicity, Enzymatic, and Antiviral Activities of Compounds 6a–l and 7a–m

					activity in enzyme assay, IC50 a		antiviral activity
compd	R	R1	R2	X	RHb	STc	EC50 d	CC50 e	SIf
6a	Ph	H	OH	Et	10	0.42	0.56	11	19.6
6b	Ph	Me	OH	Et
6c	H	H	OH	Et	>100	1.6	0.90	>50	>55
6d	Ph	H	NH2	Et	72	NT	19	>50
6e	4-FBzg	Bnh		Et	>100	4.3	19	>50
6f	4-FBzg	Ph		Et	1.8	1.2	20	>50
6g	4-FBzg	Me		Et	28	>333	48	>50
6h	Ph	4-FBnh		Et	13.4	2.5
6i	H			Et	55	90	50	>50
6j	Ph			Et	3.0	>21	4.3	26.9	6.3
6k	H			COOEt	21	0.51	1.2	33	27
6l	Ph			COOEt	6.0	0.79	0.70	3.9	6
7a	Ph	H	OH	H	7.5	0.022	0.66	>50	>75
7b	Ph	CH3	OH	H	64	>111	>50	>50
7c	H	H	OH	H	41	0.024	0.58	>50	>86
7d	Ph	H	NH2	H	2.0	0.043	0.63	>50	>79
7e	4-FBzg	Bnh		H	7.5	0.063	>50
7f	4-FBzg	Ph		H	100	0.59	>50
7g	4-FBzg	Me		H	20
7h	Ph	4-FBnh		H	23	0.066
7i	H			H	69	26	>50	>50
7j	Ph			H	7.0	0.73	17.2	>50	>2.9
7ki	H			COOH	54	0.057	1.0	28	28
7l	Ph			COOH	14	0.019	0.7	>50	>72
7m	H			Trj	26	0.11	20.4	>50
1						0.007	0.016	>250	>15000
2					3.2	1.9	>50
3					8	98	<0.2	>50	>250
4					3	0.60	2	>50	>25
5					26.2	2.4	3.6	>50	>13.8

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

^bExperiments performed against HIV-1 RT-associated RNase H activity.

^cExperiments performed against HIV-1 IN ST activity.

^dEffective concentration 50% (μM).

^eCytotoxic concentration 50% (μM).

^fSI = CC₅₀/EC₅₀.

^gBz, benzoyl.

^hBn, benzyl.

ⁱSee also ref 33.

^jTr, triazolyl.