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

Authors
Journal
European Journal of Medicinal Chemistry
0223-5234
Publisher
Elsevier
Identifiers
DOI: 10.1016/j.ejmech.2014.09.053
Keywords
  • Combretastatin A-4
  • Pironetin Analogues
  • Hybrid Molecules
  • Click Reaction
  • Tubulin-Active Compounds
  • Cytotoxicity

Abstract

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.

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