. 2021 Jun 2;64(12):7926–7962. doi: 10.1021/acs.jmedchem.0c02265

Table 3. Summary of Chemical Classification, Cancer Cell Lines, and Assays Used for the Biological Evaluation of the Most Representative σR Ligands.

Compound	Chemotype	Cell line	Biological test	Reference
σ₁R Ligands
1	N,N-dialkyl and N-alkyl-N-aralkyl fenpropimorph-derivatives	NCI-H460, DU145, MCF7, SKOV-3, MB-MDA231	multiplex cytotoxicity assays	(101)
2		SKOV-3
5		MCF-7
13, 14	spipethiane derivatives	MCF-7/ADR	annexin V-FITC assay, tail-flick assay
20, 21	spirocyclic thienopyran and thienofuran derivatives	A427	retinal ganglion assay, capsaicin assay, crystal violet assay, LDH assay	(83, 111, 113, 178)
36	7,9-diazabicyclo[4.2.2]decane derivative	A427	crystal violet assay	(131)
ent-38, 40, ent-40, ent-41, 42, ent-42	2,5-diazabicyclo[2.2.2]octane derivatives	A427	crystal violet assay, annexin V-FITC assay	(132)
ent-38, 39, ent-41, 42	2,5-diazabicyclo[2.2.2]octane derivatives	5637	crystal violet assay, annexin V-FITC assay	(132)
σ₂R Ligands
SWIII-123	granatane derivative	SKOV-3, CaOV-3, BG-1	MTS assay	(146)
49	indole derivatives	MCF-7, MCF-7/dox, DU145, C6, A549/DX	MTT assay, cell cycle analysis	(158, 159, 162)
51	indole derivatives	DU145, MCF-7, C6	MTT assay, cell cycle analysis	(159)
F281	carbazole derivative	Panc02	MTT assay	(36)
PB221	tetralin derivative	Panc02, ALTS1C1, UN-KC6141	MTT assay, caspase-Glo assay	(36, 79)
CM572, CM764	1,3-benzoxazol-2(3H)-one derivatives	SK-N-SH	MTT assay	(112, 166)
66	6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivative	Huh-7, KYSE-140	CCK8 assay	(170)
86	3-alkoxyisoxazole derivative	143B, MOS-J	crystal violet assay, annexin V assay	(176)