Table 1 Overview of studies investigating the effect of G4 ligands on different melanoma cell lines

5ME

B16F10_m

48 h

IC₅₀: ~100 μM

x

[122]

Ant1,5

SKMel-5_h, ROSS_h, A375_h, M14_h

48 h

IC₅₀: 4 μM (ROSS) to 10 μM (SCMel-5)

x

[123]

BRACO19

B16_m

24 h

IC₅₀: 28 μM

x

[124]

C8

B16_m

72 h

IC₅₀: ~5 μM

x

[125]

C14

Derivate from TMPyP4; induces singlet oxygen (¹O₂) production

B78-H1_m

n.a.

In vitro:

IC₅₀ (metabolic activity): 10 nM

In vivo:

About 50% tumor growth reduction.

x

[121]

c-exNDIs

A375_h, SK-MEL-2_h

48 h

IC₅₀: ~8 nM

x

[126]

CORON

M14h, LOX IMVI_h, MALME-3M_h, SK-MEL-2_h, SK-MEL-28_h, SK-MEL-5_h, UACC-62_h

n.a.

LC₅₀: mean for all cell lines ~2.5 μM

x

x

x

[127, 128]

CX-3543 (Quarfloxin)

M14_h, MALME-3M_h, UACC-257_h, UACC-62_h

n.a.

IC₅₀: > 1 μM for all cell lines

x

x

[129]

EMICORON

M14_h, LOX IMVI_h, MDA-MB-435_h, SK-MEL-2_h, SK-MEL-28_h, SK-MEL-5_h, UACC-62_h, UACC-257_h

n.a.

LC₅₀: mean for all cell lines ~3 μM

x

x

x

[127, 128]

IZCZ-0

A375_h

24 h

IC₅₀: 2.3 μM

x

[130]

IZCZ-3

A375_h

24 h

IC₅₀: 4.2 μM

x

[130]

IZTC-1

B16_m

24 h

IC₅₀: ~2.2 μM, ~50-65% reduced melanoma growth in vivo. Binds preferentially to MYC G4

x

[124]

N,N'-bis(3,4-dihydroxbenzy lidene)-1,2-diaminobenzene (crosslinker)

B16F1_m

n.a.

x

[131]

Naphthalene diimide derivatives

(compound 2)

SKMEL-5_h

48 h

IC₅₀: 1.7 μM

x

x

[132]

PhenDC3

A375_h

96 h

GI₂₀: 10 μM

x

[69]

Phenyl 1,2,3-triazole-thymidine ligands

(L1, L2, L3)

B16F10_m

24 and 48 h

IC₅₀: 200 μM (L1), 125 μM (L2), 50 μM (L3)

x

[133]

PPL3C

M14_h

96 h

IC₅₀: 0.8 μM

x

[128, 134]

Pyridostatin

A375_h

96 h

GI₂₀: 1.5 μM

x

[69]

RHPS4

M14_h, PLF2_h, JR1_h, JR8_h, SBCL1_h, SAN_h, LP_h, LM_h, JR5_h, M14_h

5 and 7 days

IC₅₀: 3.1 μM (5 days M14), ~1 μM (5 days PLF2_h, JR1, JR8, SBCL1, SAN)

~1 μM (7 days M14, PLF2_h, JR1, JR8, SBCL1, SAN)

About 50% reduced tumor growth in melanoma xenografts

x

[135,136,137]

TMPyP4

B78-H1_m

48 h

IC₅₀ (metabolic activity): 200 nM

IC₅₀: 85 μM

~65% reduced tumor growth in vivo (+ light therapy)

x

[121, 122]

trans-resveratrol (tRES)

M14_h, SKMEL-28_h

48 and 72 h

IC₅₀: 5 μM (M14, 48 h), 2.5 μM (SKMEL-28, 48 h) IC₅₀: ~25 μM (SKMEL-28, 72 h)

x

x

[138, 139]

Trisubstituted naphthalimides (compounds VII, VIII and IX)

M14_h

5 days

IC₅₀: ~1.5 μM (VII), ~34.7 μM (IX)

x

[140]