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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Pyridine Based Antitumour Compounds Acting at the Colchicine Site

Author(s): R. Álvarez, L. Aramburu, P. Puebla, E. Caballero, M. González, A. Vicente, M. Medarde and R. Peláez

Volume 23 , Issue 11 , 2016

Page: [1100 - 1130] Pages: 31

DOI: 10.2174/092986732311160420104823

Price: $65


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.

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