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Table 3 Small-molecule compounds targeting other RCD subroutines in TNBC

From: Targeting regulated cell death (RCD) with small-molecule compounds in triple-negative breast cancer: a revisited perspective from molecular mechanisms to targeted therapies

Chemical structure

Name in the literature

Target

Mechanism in RCD

Activity

TNBC subtype

References

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PTX

Microtubule inhibitor

Active mitotic catastrophe

MDA-MB-231 (IC50 = 5.78 μM)

Hs578T (IC50 = 0.15 μM)

MSL

[199]

JQ1

BET inhibitor

Active mitotic catastrophe

MDA-MB-231 (50 nM)

HCC70 (500 nM)

HCC1143 (200 nM)

BL1

MSL

[193, 205]

SB218078

Chk1 inhibitor

Active mitotic catastrophe

HCC1937 (IC50 > 10 μM)

IGRBr-11 (IC50=8.56 μM)

BL1

UNS

[208]

Torin2

mTOR and PIKKs inhibitor

Active mitotic catastrophe

HCC1806 (GR50 = 0.08 μM)

HCC70 (GR50 = 0.02 μM)

BL2

[214]

KX-01

SRC and tubulin inhibitor

Active mitotic catastrophe

MDA-MB-231 (IC50 = 0.0446 ± 0.0009 μM)

MDA-MB-468 (IC50 = 0.0613 ± 0.0017 μM)

BT-549 (IC50 = 0.0467 ± 0.0019 μM)

BL1

M

MSL

[215]

erastin@FA-exo

Ferroptosis inducer

Active ferroptosis

MDA-MB-231 (IC50 = 10 μM)

MSL

[248]

As4O6

Tetraarsenic hexoxide (As4O6)

STAT3 inhibitor

Active pyroptosis

Hs578T (IC50 > 10 μM)

MDA-MB-231 (IC50 = 5 μM)

MSL

[258]

Cisplatin

Activation of MEG3/NLRP3/caspase-1/GSDMD Pathway

Active pyroptosis

MDA-MB-231 (IC50 = 9.952 nM)

MSL

[260]

AEB071

PKCθ inhibitor

Active anoikis

MDA-231-Luc-D3H2LN (IC50 = 500 nM)

 

[268]

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Synthesized flavonoid derivative GL-V9

Glucose-6-phosphate dehydrogenase (G6PD)↓

Phospho-acetyl-CoA carboxylase (p-ACC)

AMPK↑

Active anoikis

MDA-MB-231 (IC50 = 20 μM)

MSL

[271]

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Tubeimoside V (TBMS-V)

EGFR↑

ITGB1-FAK↑

Active anoikis

MDA-MB-231 (IC50 = 2.5 μM)

MSL

[272]

Disulfiram/copper (DSF/Cu)

Calpain and decomposing vimentin in a Cu-dependent manner↑

Active anoikis

MDA-MB-231 (IC50 = 1 μM)

Hs578T (IC50 = 1 μM)

MSL

[274]

Salinomycin

STAT3 inhibitor

Active anoikis

MDA-MB-231 (IC50 = 10 μM, 72 h)

MSL

[286]

 

POL5551

CXCR4 inhibitor

Active anoikis

 

MSL

[294]

AL10

Sialyltransferase inhibitor

Active anoikis

MDA-MB-231 (IC50 = 10 μM)

MSL

[296]

Berberine (BBR)

 

Active anoikis

MDA-MB-231 (IC50 = 10 μM)

MSL

[276]

HPW-RX40

Integrin inhibitor

Active anoikis

MDA-MB-231 (IC50 = 15.2 μM)

MSL

[297]

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Archazolid A

V-ATPase inhibitor

Active and inhibit anoikis

MDA-MB-231 (10 nM)

MSL

[298]

Narciclasine

Upregulate AMPK-ULK1 pathway

Active autophagy-dependent cell death and apoptosis

HCC‐1937 (IC50 = 0.25 μM)

MDA-MB-231 (IC50 = 0.5 μM)

BT-579 (IC50 = 2 μM)

BL1

M

MSL

[305]

Compound 7C (3-bromo-N'-(4-hydroxybenzylidene)-4-methylbenzohydrazide derivatives)

mTOR inhibitor

Active autophagy-dependent cell death and apoptosis

MDA-MB-231 (IC50 = 3.38 ± 1.01 μM)

MDA-MB-468 (IC50 = 4.30 ± 1.82 μM)

BL1

MSL

[306]

Cantharidin

Beclin1 inhibitor

Inhibit autophagy-dependent cell death and active apoptosis

MDA-MB-231 (IC50 = 10 µg/ml)

MDA-MB-468 (IC50 = 10 µg/ml)

BL1

MSL

[307]

Eupalinolide G

Eupalinolide I

Eupalinolide J

F1012-2

Active Akt and p38 pathway

Inhibit autophagy-dependent cell death and active apoptosis

MDA-MB-231 (IC50 = 6.76 ± 0.42 µg/ml)

MDA-MB-468 (IC50 = 6.23 ± 0.32 µg/ml)

 

[308]

Flubendazole

EVA1A activator

Active autophagy-dependent cell death and apoptosis

MDA-MB-231 (IC50 = 0.623 μM)

MDA-MB-468 (IC50 = 0.728 μM)

BLC1

MSL

[310]

CSC-3436

AMPK/mTOR pathway ↓

Active autophagy-dependent cell death and apoptosis

MDA-MB-231 (IC50 = 205 ± 3.21 nm for 48 h, IC50 = 148 ± 2.31 nm for 72 h)

MSL

[313]

Jatamanvaltrate P

Cleavage of PARP and caspases ↑;

Cell cycle-related Cyclin B1, Cyclin D1 and Cdc-2 ↓

Active autophagy-dependent cell death and apoptosis

MDA-MB-231 (IC50 = 4.32 ± 1.34 µM)

MDA-MB-468 (IC50 = 7.05 ± 2.51 µM)

MDA-MB-453 (IC50 = 4.05 ± 0.18 µM)

BL1

MSL

LAR

[314]

1,4,5-Oxathiazinane-4,4-dioxide (OTD)

 

Active necroptosis and apoptosis

BT-20 (IC50 = 500 μM)

MDA-MB-231 (IC50 = 200 μM)

MSL

UNS

[315]

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AEZS 126

PI3K/AKT inhibitor

Active necroptosis and apoptosis

HCC1937 (IC50 = 3.2 μM)

BL1

[318]

Azobenzene combretastatin A4 (Azo-CA4)

Microtubule inhibitor

Active ferroptosis and apoptosis

MDA-MB-231 (IC50 = 1.02 mg/mL)

MSL

[331]

DMOCPTL

GPX4 inhibitor

Active ferroptosis and apoptosis

MDA-MB-231 (IC50 = 0.34 ± 0.13 μM)

MSL

[320]