Synthesis and biological activity of fluorinated combretastatin analogues

…, G Gallo, MO Tinti, M Marcellini, T Riccioni…

Index: Alloatti, Domenico; Giannini, Giuseppe; Cabri, Walter; Lustrati, Isabella; Marzi, Mauro; Ciacci, Andrea; Gallo, Grazia; Tinti, M. Ornella; Marcellini, Marcella; Riccioni, Teresa; Guglielmi, Mario B.; Carminati, Paolo; Pisano, Claudio Journal of Medicinal Chemistry, 2008 , vol. 51, # 9 p. 2708 - 2721

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Citation Number: 47

Abstract

With the aim of understanding the influence of fluorine on the double bond of the cis-stilbene moiety of combretastatin derivatives and encouraged by a preliminary molecular modeling study showing a different biological environment on the interaction site with tubulin, we prepared, through various synthetic approaches, a small library of compounds in which one or both of the olefinic hydrogens were replaced with fluorine. X-ray analysis on the difluoro ...