2. Academic Validation
  3. Design and synthesis of pironetin analogue/combretastatin A-4 hybrids containing a 1,2,3-triazole ring and evaluation of their cytotoxic activity

Design and synthesis of pironetin analogue/combretastatin A-4 hybrids containing a 1,2,3-triazole ring and evaluation of their cytotoxic activity

  • Eur J Med Chem. 2014 Nov 24:87:125-30. doi: 10.1016/j.ejmech.2014.09.053.
Concepción Vilanova 1,  Sandra Torijano-Gutiérrez 1,  Santiago Díaz-Oltra 1,  Juan Murga 2,  Eva Falomir 1,  Miguel Carda 1,  J Alberto Marco 3
Affiliations

Affiliations

  • 1 Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain.
  • 2 Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain. Electronic address: jmurga@qio.uji.es.
  • 3 Depart. de Q. Orgánica, Univ. de Valencia, E-46100 Burjassot, Valencia, Spain. Electronic address: alberto.marco@uv.es.
PMID: 25240870 DOI: 10.1016/j.ejmech.2014.09.053
Abstract

We here describe the preparation of a series of hybrid molecules containing a combretastatin A-4 moiety and a pironetin analogue fragment connected through a spacer of variable length which includes a 1,2,3-triazole ring. The cytotoxic activities of these compounds have been measured. Relations between structure and cytotoxicity are discussed. Some of the tested compounds showed cytotoxicity values of the same order of magnitude as combretastatin A-4 and were less toxic than the latter compound for normal cells.

Keywords

Click reaction; Combretastatin A-4; Cytotoxicity; Hybrid molecules; Pironetin analogues; Tubulin-active compounds.

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