Synthesis and anticancer activity of analogues of phenstatin, with a phenothiazine A-ring, as a new class of microtubule-targeting agents

…, P Gautret, D Belei, A Farce, J Dubois, A Ghinet

Index: Abuhaie, Cristina-Maria; Bicu, Elena; Rigo, Benoit; Gautret, Philippe; Belei, Dalila; Farce, Amaury; Dubois, Joelle; Ghinet, Alina Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 1 p. 147 - 152

Full Text: HTML

Citation Number: 18

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 93nM on ...