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Design and Synthesis of Pironetin Analogue/Combretastatin A‐4 Hybrids and Evaluation of Their Cytotoxic Activity
Author(s) -
TorijanoGutiérrez Sandra,
Vilanova Concepción,
DíazOltra Santiago,
Murga Juan,
Falomir Eva,
Carda Miguel,
Marco J. Alberto
Publication year - 2014
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.201301725
Subject(s) - combretastatin , chemistry , moiety , cytotoxicity , stereochemistry , cytotoxic t cell , molecule , in vitro , organic chemistry , biochemistry , tubulin , microtubule , biology , microbiology and biotechnology
We describe the preparation of a series of hybrid molecules containing a combretastatin A‐4 moiety and a pironetin analogue fragment linked by an ester spacer of variable length. The cytotoxic activities of these compounds have been measured and the relationship between the structure and cytotoxicity is discussed. Some of the tested compounds showed cytotoxicity values of the same order of magnitude as those of the parental molecules, combretastatin A‐4 and pironetin, and were less toxic than the latter for normal cells.