Pyridine Based Antitumour Compounds Acting at the Colchicine Site

R. Álvarez, L. Aramburu, P. Puebla, E. Caballero, M. González, A. Vicente, M. Medarde, R. Peláez
2016 Current Medicinal Chemistry  
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
more » ... ic compounds are described. The design 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.
doi:10.2174/092986732311160420104823 pmid:27117490 fatcat:wfuurrmhyrd3ncz5fqdaape2vq