Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596139 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
A new family of microtubule-targeting agents with a phenothiazine A-ring was synthesized and evaluated for anti-proliferative activity and interaction with tubulin. These new derivatives showed significant activities against cellular proliferation and tubulin polymerization, rather similar to those of phenstatin. Phenothiazine derivative 21 proved to be the most potent compound synthesized with GI50 values ranging from 29 to 93Â nM on different cell lines. The same compound showed a better inhibition of COLO 205, A498, and MCF7 cell lines than the parent phenstatin.
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Authors
Cristina-Maria Abuhaie, Elena Bîcu, Benoît Rigo, Philippe Gautret, Dalila Belei, Amaury Farce, Joëlle Dubois, Alina Ghinet,