. Author manuscript; available in PMC: 2020 May 9.

Published in final edited form as: J Med Chem. 2019 Apr 30;62(9):4669–4682. doi: 10.1021/acs.jmedchem.9b00274

Table 5.

Cytotoxicity evaluation in two cell lines.

Compd	CC₅₀ (μM)^a		PAMPA P_e (10⁻⁶ cm/s)^b	Compd	CC₅₀ (μM)^a		PAMPA P_e (10⁻⁶ cm/s)^b
Compd	HepG2	HeLa	PAMPA P_e (10⁻⁶ cm/s)^b	Compd	HepG2	HeLa	PAMPA P_e (10⁻⁶ cm/s)^b
4a^d	>100	>100	0.003	11i	14	12	2.7
4b^d	>100	--	0.01	11j	8.7	9.4	0.7
4c^d	>100	--	0.008	11k	>100	>100	0.003
4d^d	>100	--	0.4	11l	25	30	1.7
4e	40	28	1.1	11m	9.0	21	2.0
4f	85	79	0.3	12a	50	>100	0.1
4g	>100	>100	0.5	12b	41	45	0.08
4h	42	39	1.1	12c	46	32	0.06
31	>100	>100	0.1	12d	49	67	0.05
11a	14	12	1.2	12e	>100	--	0.03
11b	>100	>100	0.4	12f	>100	--	0.01
11c	17	--	0.2	12g	85	65	0.04
11d	14	12	0.4	12h	82	90	0.07
11e	29	29	0.6	12i	42	62	0.03
11f	>100	>100	0.01	12j	>100	>100	0.02
11g	29	--	2.8	12k	>100	>100	0.06
11h	5.3	7.4	0.8	12l	33	25	4.4

CC₅₀: concentration of a compound causing 50% cell death. ETP was used as control: CC₅₀ = 15 μM (HepG2) and 17 μM (HeLa).

P_e: effective permeability coefficients determined using the PAMPA, measured in five replicates.