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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