Abstract
Antimitotics binding at the colchicine site of tubulin are important antitumour and vascular disrupting agents. Pyridines and azines are privileged scaffolds in medicinal chemistry and in recent years many colchicine site ligands (CSL) have incorporated them into their structures with the aim of improving their pharmacokinetic and pharmacodynamics properties. CSL have been classified according to their chemical structures and the chemical structures of the pyridine and azine containing antimitotic compounds are described. The designed principles behind the structural modifications and the achieved effect on the biological activity upon inclusion of these heterocycles are also discussed. Lessons from the achievements and failures have been extracted and future perspectives delineated.
Keywords: Pyridine, azines, antimitotics, tubulin, colchicine, antitumour, drug design.
Current Medicinal Chemistry
Title:Pyridine Based Antitumour Compounds Acting at the Colchicine Site
Volume: 23 Issue: 11
Author(s): R. Álvarez, L. Aramburu, P. Puebla, E. Caballero, M. González, A. Vicente, M. Medarde and R. Peláez
Affiliation:
Keywords: Pyridine, azines, antimitotics, tubulin, colchicine, antitumour, drug design.
Abstract: Antimitotics binding at the colchicine site of tubulin are important antitumour and vascular disrupting agents. Pyridines and azines are privileged scaffolds in medicinal chemistry and in recent years many colchicine site ligands (CSL) have incorporated them into their structures with the aim of improving their pharmacokinetic and pharmacodynamics properties. CSL have been classified according to their chemical structures and the chemical structures of the pyridine and azine containing antimitotic compounds are described. The designed principles behind the structural modifications and the achieved effect on the biological activity upon inclusion of these heterocycles are also discussed. Lessons from the achievements and failures have been extracted and future perspectives delineated.
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Cite this article as:
Álvarez R., Aramburu L., Puebla P., Caballero E., González M., Vicente A., Medarde M. and Peláez R., Pyridine Based Antitumour Compounds Acting at the Colchicine Site, Current Medicinal Chemistry 2016; 23 (11) . https://dx.doi.org/10.2174/092986732311160420104823
DOI https://dx.doi.org/10.2174/092986732311160420104823 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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