Skip to main content
. Author manuscript; available in PMC: 2008 Nov 20.
Published in final edited form as: J Med Chem. 2007 Jan 31;50(4):713–725. doi: 10.1021/jm061071x

Table 1.

Cytotoxicity and tubulin polymerization activity of macrocyclic and open chain paclitaxel analogs.

Compound IC50 values (nM)a,b
 Tubulin polym (ED50, µM)b,g
A2780 PC3
PTX 15c 5 0.5
13a 1900 550 1.0
13b 1700 320 1.0
13c 17800 2800c 1.2c
13d 19800 >13200 2.7c
13e 1600c 275 1.4
13f 1300e 550 1.4
13g 770c 128 0.42
13h 350 55 0.49
13i 2520 2600 1.8
13j 7400 4600c 2.2
15a 6300 580 4.6c
15c 14.5 15 0.28
15d 20d 16 0.67
15f 0.3d 2.5 0.3
15g 650 NDf NDf
15h 680 34 1.6
15i 830 55 0.9
15j 440 90 0.53
15k 1840c 500 0.93
18f 0.5d 3.1 0.33
16a 700d 53 1.4
16c 18.5d 50c 0.83
16d 28 13 0.23
16f 0.5d 2.4 0.21
16g 3600c 1000 3.4c
16h 8800 570 1.4
16i 980c 51 0.76
16j 2000 390c 0.85
25 23.7d 6 0.57h
26 23.1e NDf NDf
28 17.7d 8.2 0.22h
31a 1.4d 3.2 0.49h
31b >6i 11 0.35h
32a 0.65d 1.5 0.18h
32b 0.49d 1.3 0.22h
a

Average of three determinations unless otherwise stated

b

Standard error is less than 10% of the mean unless otherwise stated.

c

Standard error between 10% and 25% of the mean.

d

Standard error greater than 25% of the mean.

e

Single determination

f

ND: Samples were not tested.

g

ED50 values determined with GTP-tubulin unless otherwise stated.

h

ED50 values for these samples were determined with GDP-tubulin and were normalized to the GTP-tubulin scale.

i

The value cited is the lower of two widely different determinations, probably due to solubility problems.