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The Mechanism of the Interactions of Pironetin Analog/Combretastatin A‐4 Hybrids with Tubulin
Author(s) -
TorijanoGutiérrez Sandra,
Vilanova Concepción,
DíazOltra Santiago,
Murga Juan,
Falomir Eva,
Carda Miguel,
RedondoHorcajo Mariano,
Díaz José Fernando,
Barasoain Isabel,
Marco Juan Alberto
Publication year - 2015
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201500106
Subject(s) - tubulin , combretastatin , microtubule , moiety , chemistry , mechanism of action , stereochemistry , molecule , cell culture , biophysics , biochemistry , in vitro , microbiology and biotechnology , biology , organic chemistry , genetics
We here report an investigation of the interactions with tubulin of two types of molecules of a hybrid structural type consisting in a combretastatin A‐4 moiety and a simplified pironetin fragment. The cytotoxicities of the molecules on two reference tumoral cell lines were measured. In addition, the effects of the compounds on the cell cycle and on microtubule assembly were observed. The dynamics of microtubule polymerization was investigated by means of immunofluorescence assays. It was thus established that at least some of the compounds under study exert their cytotoxic action by means of interaction with tubulin.