Table 1 Characteristics of 21 active compounds ¹ against NCI-H295R cells with efficacy higher than 60% and potency below 0.9 μM

Aclarubicin

IV

0.94

0.34

13.3 hrs

-122.30

Topoisomerase I and II inhibitor

Actinomycin D

IV

0.38

0.02-0.08

36 hrs

-112.51

Inhibitors of DNA synthesis

Bortezomib

IV

0.34

0.16-0.31

9-15 hrs

-77.11

Proteasome inhibitor;

Carboquone

PO/IV

0.75

0.62-0.74 (200-240 ng/mL)

0.5 hrs

-119.79

Alkylating agents

Ciclopirox

Topical

0.64

N/A - topical only

2.2 hrs in rabbits

-61.11

Chelation of polyvalent metal cations

Deslanoside

0.34

0.16

51 hrs

-110.35

Na+/K + ATPase inhibition;

Digitoxin

IV

0.08

0.05-0.2

4-9 days

-109.13

Na+/K + ATPase inhibition;

Digoxin

PO/IV

0.19

0.003

36-48 hrs

-111.40

Na+/K + ATPase inhibition;

Ecteinascidin

IV

0.01

Up to 0.05

50-180 hrs

-116.82

Disruption of DNA strand

Homoharringtonine

SQ

0.21

0.176

9.3 hrs

-125.33

Protein synthesis inhibitor

Lanatoside A

IV/PO

0.19

N/A

N/A

-114.10

Na+/K + ATPase inhibition;

Lanatoside C

IV/PO

0.3

N/A

N/A

-117.82

Na+/K + ATPase inhibition;

Methotrexate

PO/IV

0.02

10-100

8-15 hrs

-74.91

DHFR inhibitor

Metildigoxin

PO/IV

0.24

N/A

N/A

-110.90

Na+/K + ATPase inhibition;

Niclosamide

PO/IV

0.27

N/A

N/A

-94.29

Uncouple oxidative phosphorylation

Ouabain

IV

0.08

0.128

18 hrs

-110.64

Na+/K + ATPase inhibition;

Plicamycin

IV

0.94

0.6 μM

10.5 hrs

-117.62

RNA synthesis inhibitor;

Proscillaridin A

IV/PO

0.01

0.019 (IV); 0.0019 (PO)

23-33 hrs

-110.55

Na+/K + ATPase inhibition;

Pyrimethamine

PO/IV

0.75

8.04

140-190 hrs

-81.43

DHFR inhibitor

Rotenone

N/A

0.75

N/A

N/A

-69.22

Electron transport chain in mitochondria interference

Trimetrexate glucuronate

IV

0.01

N/A

11-16 hrs

-80.39

DHFR inhibitor