Table 1.

Structure and HIV-1 integrase inhibitory activities of chalcones

IC50(μM)				Activity
Comp.	Ar	X	R1	3′-Pa	STb
10	Ph	COOH	Br	75 ± 14	25 ± 5
11	2-Cl-Ph	COOH	Br	52 ± 13	14 ± 4
12	2-F-Ph	COOH	Br	74 ± 25	32 ± 3
13	3-Cl-Ph	COOH	Br	45 ± 10	9 ± 3
14	4-Cl-Ph	COOH	Br	81 ± 28	12 ± 1
15	4-Br-Ph	COOH	Br	11 ± 4	5 ± 2
16	4-I-Ph	COOH	Br	69	35
17	2,4-di-Cl-Ph	COOH	Br	28 ± 12	7 ± 4
18	2,3-di-Cl-Ph	COOH	Br	58 ± 13	19 ± 11
19	2,3,di-MeO-Ph	COOH	Br	62 ± 14	34 ± 6
20	2,3,4-tri-MeO-Ph	COOH	Br	85 ± 20	51 ± 16
21	2,5-di-Cl-Ph	COOH	Br	47 ± 14	18 ± 4
22	2,6-di-Cl-Ph	COOH	Br	52 ± 12	16 ± 8
23	3,4-di-Cl-Ph	COOH	Br	27 ± 11	14 ± 4
24	2,3,5-tri-Cl-Ph	COOH	Br	20 ± 12	13 ± 5
25	2,3,6-tri-Cl-Ph	COOH	Br	23 ± 12	<3.7
26	4-Cl-Ph	COOH	Cl	85 ± 13	53 ± 21
27	2,4-di-Cl-Ph	COOH	Cl	> 100	> 100
28	2,3-di-Cl-Ph	COOH	Cl	100	92 ± 14
29	2,5-di-Cl-Ph	COOH	Cl	75	25
30	2,3,5-tri-Cl-Ph	COOH	Cl	55 ± 40	17 ± 3
31	2,3,6-tri-Cl-Ph	COOH	Cl	77 ± 20	30 ± 5
32	3,4-di-Cl-Ph	COOH	Cl	87 ± 13	41 ± 9
33	4-Cl-Ph	COOH	F	36 ± 13	17 ± 3
34	2,4-di-Cl-Ph	COOH	F	52 ± 13	24 ± 9
35	2,3-di-Cl-Ph	COOH	F	55 ± 18	30 ± 9
36	2,5-di-Cl-Ph	COOH	F	50	29 ± 6
37	2,3,5-tri-Cl-Ph	COOH	F	33 ± 14	15 ± 4
38	2,3,6-tri-Cl-Ph	COOH	F	82 ± 16	39 ± 6
39	3,5-di-Me-Ph	COOH	Br	>100	58
40	2-Cl-3,4-di-MeO-Ph	COOH	Br	>100	76
41	6-F-3,4-di-MeO-Ph	COOH	Br	>100	76
42	2-BzO-Ph	COOH	Br	21	9
43	3-(4-Cl-PhO)-Ph	COOH	Br	25	18
44	4-(4-Cl-PhO)-Ph	COOH	Br	22	16
45	3-thienyl	COOH	Br	30 ± 12	18 ± 1
46	3-(cyclopentyloxy)-Ph	COOH	Br	100	55
47	3-(2-OEt-naphthyl)	COOH	Br	92	46
48	5-MeO-naphthyl	COOH	Br	54	54 ± 25
49	5-benzothiophene	COOH	Br	23 ± 3	11 ± 1
50	2-furan-2-yl-Ph	COOH	Br	>100	16 ± 2
51	3-Cl-4,5-Methylenedioxy-Ph	COOH	Br	79	63
52	3-OCF3-Ph	COOH	Br	>100	52
53	3-NO2-Ph	COOH	Br	49 ± 8	32 ± 6
54	3-Br-Ph	COOH	Br	19 ± 4	18 ± 1
55	3-F-Ph	COOH	Br	71 ± 1	59 ± 2
56	2,3,6-tri-Cl-Ph	CN	Br	>100	44 ± 2
57	2,3,6-tri-Cl-Ph	COOH	CH3	>100	50 ± 9
58	2,3,5-tri-Cl-Ph	NO2	Br	>333	68 ± 5
59	2,3,6-tri-Cl-Ph	NO2	Br	36 ± 4	21 ± 3
S1360c	N/A	N/A	N/A	11 ± 2	0.6 ± 0.1

^a3-P = 3′-processing,

^bST = strand transfer,

^cS1360 = standard