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Updated: Aug 20, 2026

Optimizing Tubulin Yield from Porcine Brain Tissue
Published on: October 11, 2024
Arylthioindoles, potent inhibitors of tubulin polymerization
Gabriella De Martino1, Giuseppe La Regina, Antonio Coluccia
1Dipartimento di Studi Farmaceutici, Università di Roma, La Sapienza, I-00185 Rome, Italy.
Abstract:
Several arylthioindoles had excellent activity as inhibitors both of tubulin polymerization and of the growth of MCF-7 human breast carcinoma cells. Methyl 3-[(3,4,5-trimethoxyphenyl)thio]-5-methoxy-1H-indole-2-carboxylate (21), the most potent derivative, showed IC(50) = 2.0 microM, 1.6 times more active than colchicine and about as active as combretastatin A-4 (CSA4). Compound 21 inhibited the growth of the MCF-7 cells at IC(50) = 13 nM. Colchicine and CSA4 had 13 nM and 17 nM IC(50) values, respectively, with these cells.
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