. Author manuscript; available in PMC: 2019 Nov 5.

Published in final edited form as: Eur J Med Chem. 2018 Sep 21;159:217–242. doi: 10.1016/j.ejmech.2018.09.043

Table 2.

Cytotoxicity, CD98 down-regulation and vacuolation profiles of the C-2 modified variants of analog 3 (as HCl salts)

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Comp.	IC50 (μM) [95% CI]		%CD98 down-regulation			Vacuolation score

			2.5 μM	10 μM	40 μM	2.5 μM	10 μM	40 μM
3	2.1	[2.0, 2.2]	42	66	n.d.	++	+++	n.d.
8	2.5	[2.3, 2.8]	28	57	n.d.	+	+++	n.d.
9	2.8	[2.6, 3.0]	41	63	n.d.	++	+++	n.d.
10	3.0	[2.7, 3.3]	16	58	n.d.	0	+++	n.d.
11	2.1	[1.5, 2.8]	22	46	n.d.	+++	+++	n.d.
12	2.0	[1.6, 2.6]	44	60	n.d.	++	+++	n.d.
13	4.0	[3.5, 4.6]	8	46	n.d.	0	+++	n.d.
14	12.2	[11.4, 13.0]	0	32	68	0	0	+
15	2.1	[1.9, 2.3]	15	52	n.d.	++	+++	n.d.
16	2.2	[2.1,2.3]	40	63	n.d.	++	+++	n.d.