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. Author manuscript; available in PMC: 2010 Dec 10.
Published in final edited form as: J Med Chem. 2009 Dec 10;52(23):7512–7527. doi: 10.1021/jm900016t

Table 2.

Inhibition of Tubulin Polymerization, Growth of MCF-7 Human Breast Carcinoma Cells by Compounds 46–56, and Reference Compound 2graphic file with name nihms-163005-t0002.jpg

compd R1 R2 R3 X Y tubulind IC50 ± SD (μM) MCF-7a IC50 ± SD (nM)
46 COOEt H H CH2 CH >40 nd
47 COOEt H Me CH2 C-Me >40 nd
48 COOEt Me Me CH2 C-Me >40 nd
49 COOEt Et Me CH2 C-Et >40 nd
50 H COOEt H CH2 N >40 nd
51 COOEt H H C=O CH 32±0.6 >2500
52 H COOEt H C=O N >40 >2500
53 H H COOEt C=O N >40 >2500
54 COOH H H CH2 CH >40 >2500
55 COO(CH2)2O(CH2)2OH Me Me CH2 C-Me >40 nd
56 H COOH H CH2 N·HCl >40 nd
2 1.1 ± 0.1 2.5 ± 0.6
a

Inhibition of tubulin polymerization. Tubulin was 10 μM during polymerization.

b

Inhibition of growth of MCF-7 human breast carcinoma cells.