. 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 3.

Cytotoxicity, CD98 down-regulation and vacuolation profiles of the C-2 substituted α-keto and α-hydroxy pyrrolidines

graphic file with name nihms-1508910-f0016.jpg

Comp.	IC50 (μM) [95% CI]		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.
19	<40		−21	−4	33	0	0	+++
20	28.1	[26.1, 30.2]	2	9	48	0	0/+	+++
21	15.3	[14.6, 15.9]	12	51	41	0	+++	+++
22	19.6	[18.7, 20.5]	0	19	61	0	0	+++
23	18.6	[15.5, 22.3]	13	23	59	0	0	+++
24	17.1	[14.5, 20.2]	11	16	54	0	0	+++
25	3.0	[2.6, 3.5]	19	62	n.d.	+	+++	n.d.
26	1.8	[1.7, 2.0]	9	62	n.d.	0	++	n.d.