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. Author manuscript; available in PMC: 2009 Nov 15.
Published in final edited form as: Bioorg Med Chem Lett. 2008 Oct 2;18(22):5971–5974. doi: 10.1016/j.bmcl.2008.09.103

Table 1.

ED50 ratios (compound/paclitaxel) for in vitro tubulin assembly and cytoxicity.

Entry Compound Tubulin Assembly MCF7 NCI/ADR-RES
1 paclitaxel (1) 1.0 1.0 1.0
2 TX-67 (3 – C10 CO2H) 1.7 13.3 1.3
3 C10 CH2CO2H (11) 1.8 27.9 5.8
4 C7 CO2H (18) 3.8 >30.0 5.8
5 C7 CH2CO2H (23) 1.0 8.8 13.6
6 C10 CO2Me (7) 1.0 2.5 0.4
7 C7 CO2Me (19) 1.2 0.54 0.5
8 C10 CONH2 (8) 0.4 10 6.0
9 C10 CH2CONH2 (12) 1.8 10 5.3
10 C7 CONH2 (20) 0.6 3.2 0.6
11 C7 CH2CONH2 (24) 0.6 5.0 6.5
12 C10 CONHMe (9) 0.8 7.9 6.0
13 C10 CH2CONHMe (13) 1.8 2.3 >6.3
14 C7 CONHMe (21) 0.8 2.2 1.0
15 C7 CH2CONHMe (25) 0.8 3.7 3.2
16 C10 CONMe2 (10) 1.6 2.1 2.7
17 C10 CH2CONMe2 (14) 2.2 5.6 >6.3
18 C7 CONMe2 (22) 1.1 10.8 0.8
19 C7 CH2CONMe2 (26) 0.7 3.9 3.0

Paclitaxel has a mean ED50 of 3.2 nM ± 1.8 and 1.5 µM ± 1.3 in the MCF-7 and NCI/ADR-RES lines, respectively.