Table 3 Overview of studies investigating the effect of G4 ligands on different leukemia cell lines

1,8-dipyrazolcarbazole (DPC) derivatives, compound 7b

HL-60

48 h

IC₅₀: 1.2 μM

x

[193]

7-substituted-5,6-dihydrobenzo[c] acridine derivatives, compound 2b

K-562

48 h

IC₅₀: 9.2 μM

x

[194]

9-N-substituted berberine derivatives, compound 2j

HL-60

8 days

IC₅₀: ~3 μM

x

[195, 196]

12-N-Methylated 5,6-dihydrobenzo[c] acridine derivatives, compound 21c

Ramos, CA46

96 h

IC₅₀: ~5-10 μM

x

[197]

Actinomycin D

Ramos, CA46

24 h

IC₅₀: ~25 nM (Ramos), ~10 nM (CA46)

x

[198]

Alkynylplatinum(II) terpyridine complexes (1-3)

K-562

48 h

IC₅₀: 4-7.3 μM

x

[199]

APTO-253

AML:

EOL-1, HEL92.1.7, MV4-11, KG-1, SKM-1, THP-1, NOMO-1, HL-60, MOLM-13

Leukemia/ Lymphoma:

GRANTA-519, Jeko-1, Jurkat, SUDHL-6, Mino, Raji, Ramos

5 days

LC₅₀: 0.14-1.75 μM (AML), 0.057-0.52 μM (non-AML)

x

x

[181]

AQ1

HMC1.2, α155

n.a.

n.a.

x

x

[200, 201]

B5

Ramos, CA45

48 h

IC₅₀: 11.3 μM (Ramos), 21.8 μM (CA45)

x

[198, 202]

Ber8

HL-60

48 h

IC₅₀: 1.7 μM

x

x

x

[196]

BRACO-19

CLL, AML

n.a.

IC₅₀: 80 μM

[203]

C2

Ramos, CA45

48 h

IC₅₀: 1.4 μM (Ramos), >100 μM (CA45)

x

[198, 202]

CORON

CCRF-CEM, HL-60(TB), K-562, MOLT-4, RPMI-8226, SR

n.a.

LC₅₀: 0.85 μM (K-562), 1.4 μM (MOLT-4), 1.9 μM (HL-60(TB)), > 50 μM (all other)

x

x

x

[127]

CX-3543

(Quarfloxin)

A3, CCRF-CEM, D1-1, GDM-1, HL-60, I 9.2, J45-01, Jgamma-1, Jurkat, K-562, Kasumi-1, KG-1, Ku-812, MEG-01, MOLT-3, MOLT-4, MV-4-11, P116, Reh, RPMI-8226, RS4-11, SR, TF-1, THP-1

n.a.

IC₅₀: ~1 μM

-

-

[129]

D2

Ramos, CA45

48 h

IC₅₀: 11.7 μM (Ramos), 17.8 μM (CA45)

x

[198, 202]

Diquinolinyl- Pyridine Ligands

(1a-c)

K-562, HL60

72 h

IC₅₀: >50 μM (1a), 3 μM (1b), >50 μM (1c, all K-562)

IC₅₀: >50 μM (1a), 18 μM (1b), >50 μM (1c, all HL60)

x

[204]

Disubstituted quindoline derivatives, compound 74a

Raji

CCRF-CEM

U266B2

48 h

IC₅₀: 4.7 μM (Raji), 18.1 μM (CCRF-CEM), 23.0 μM (U266B2)

Xenograft of Raji cells >50% reduced tumor growth

x

[205]

DNR

K-562

48 h

96 h

IC₅₀: 0.33 μM,

0.067 μM

x

[206]

EMICORON

CCRF-CEM, HL-60(TB), K-562, MOLT-4, RPMI-8226, SR

n.a.

LC₅₀: 3.7 μM (HL-60(TB)), > 50 μM (all other)

x

x

x

[127]

GQC-05

KG-1a, CMK, TF-1

24 h

IC₅₀: >1 μM

x

x

[207]

LZ-11

HL-60

48 h

IC₅₀: 9.6 μM

x

[208]

MXR

K-562

48 h

96 h

IC₅₀: 0.411 μM

IC₅₀: 0.105 μM

x

[206]

Pegaharmine D

HL-60

72 h

IC₅₀: 3.81 μM

x

[209]

Pyrazine-based cyclometalated (C^N^pz^C)Au(III) carbene complexes, compound 2 and 3

HL-60

72 h

IC₅₀: 0.31 μM (2),

4.05 μM (3)

-

[210]

Pyridine(2,4- dihydroxybenz aldehyde dibenzyl semicarbazone) copper(II)

MOLT-4

24 h

72 h

IC₅₀: 5 μM

IC₅₀: 1.5 μM

x

[185]

QPB compound 15e

HL-60

48 h

IC₅₀: 1.7 μM

x

[211]

Quinolino-benzo- [5, 6]-dihydro isoquindolium compounds 3a, 3f, 3g, 3j

HL-60

48 h

IC₅₀: 2 μM (3j) - 12.6 μM (3g)

x

[212]

TMPyP4

K-562, OCI-AML2, OCI-AML3

48 and 96 h

IC₅₀: 100-170 μM (K-562, 48 h), 60 μM (OCI-AML2, 96 h), 50 μM (OCI-AML3, 96 h)

x

[182, 191, 213, 214]

Telomestatin

Primary blast cells from AML patients

OM9;22, K-562

10-30 days

IC₅₀: 5 μM (10 days), 2 μM showed growth inhibition (15/30 days)

x

x

[62, 184, 215]

Substituted salicylaldehyde dibenzyl semicarbazones copper(II) complexes (7, 9, 7-py and 9-py)

MOLT-4

24 h

IC₅₀: 3.1 μM (9-py), 18.1 μM (7-py), 5 μM (7), 8.03 μM (9)

x

[215]

Sysu12d

CA46, HL-60

48 h

IC₅₀: 11.2 μM (CA46), 5 μM (HL-60)

x

x

[216]

SYUIQ-5

K-562, HL-60

72 h

IC₅₀: 5 μM (K-562, HL-60) or 2.65 μM (K-562)

x

x

x

[180, 217]

SYUIQ-FM05

K-562

24 h

IC₅₀: 10.83 nM

x

[218]