. Author manuscript; available in PMC: 2017 Apr 28.

Published in final edited form as: J Med Chem. 2016 Apr 6;59(8):3635–3649. doi: 10.1021/acs.jmedchem.5b01718

Table 4.

In vitro activity of second generation ITZ analogues.

Compound	IC₅₀ (μM)^a		GI₅₀ (μM)^a	GI₅₀ (μM)^a
Compound	C3H10T1/2^b	ASZ^c	HUVEC	MERPMB^c

12	0.091 ± 0.02	0.077 ± 0.01	3.32 ± 0.55	2.0 ± 1.3
13	0.85 ± 0.1	0.071 ± 0.02	3.69 ± 1.1	2.9 ± 1.9
14	1.1 ± 0.17	2.5 ± 0.7	7.7 ± 4.4	ND
15	>10	0.55 ± 0.07	78.3 ± 17.3	ND
16	0.47 ± 0.001	0.38 ± 0.07	18.3 ± 11.8	ND
17	1.85 ± 0.09	0.15 ± 0.038	2.5 ± 0.7	0.39 ± 0.2
18	0.54 ± 0.24	0.13 ± 0.04	12.1 ± 4.7	ND
19	6.6 ± 0.3	2.8 ± 0.9	65.0 ± 11.5	ND
20	0.19 ± 0.04	0.022 ± 0.01	53.2 ± 25.2	0.6 ± 0.2
21	2.4 ± 0.6	0.024 ± 0.02	12.8 ± 2.9	1.0 ± 0.5
22	4.1 ± 1.5	1.3 ± 0.65	26.5 ± 3.5	ND
23	>10	1.4 ± 0.5	49.9 ± 15.9	ND
24	>10	0.2 ± 0.08	84.1 ± 33.5	22.4 ± 12
25	>10	0.54 ± 0.06	24.9 ± 2.2	ND
PSZ	0.14 ± 0.02	0.54 ± 0.05	1.6 ± 0.02	1.5 ± 0.3

IC₅₀ and GI₅₀ values represent the Mean ± SEM of at least two separate experiments performed in triplicate.

All analogues evaluated following 24 hr incubation.

All analogues evaluated following 48 hr incubation.