Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles |
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Authors: | Romagnoli Romeo Baraldi Pier Giovanni Jung M Katherine Iaconinoto Maria Antonietta Carrion Maria Dora Remusat Vincent Preti Delia Tabrizi Mojgan Aghazadeh Francesca Fruttarolo De Clercq Erik Balzarini Jan Hamel Ernest |
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Affiliation: | Dipartimento di Scienze Farmaceutiche, Universitá di Ferrara, Via Fossato di Mortara 17/19, 44100 Ferrara, Italy. rmr@unife.it |
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Abstract: | A new series of compounds, in which the 2-amino-4-methoxyphenyl ring of phenstatin analogue 5 was replaced with 2- or 3-amino-benzoheterocycles, was synthesized and evaluated for antiproliferative activity and inhibition of colchicine binding. The lack of activity of 3',4'-dimethoxy- and 4'-methoxy-benzoyl derivatives (8 and 9, respectively) indicates that the 3',4',5'-trimethoxybenzoyl moiety is critical for the activity. Two compounds, 7 and 11, displayed potent antiproliferative activity, with IC50 values ranging from 25 to 100 nM against a variety of cancer cell lines. Derivative 11 was more active than CA-4 as an inhibitor of tubulin polymerization. The results demonstrated that the antiproliferative activity was correlated with inhibition of tubulin polymerization. |
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