吡啶类秋水仙中抗肿瘤化合物作用

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, R. Peláez

Affiliation:

关键词: 吖嗪、吡啶、抗有丝分裂物质，微管蛋白，秋水仙碱、抗肿瘤、药物设计。

摘要: 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.

Cite this article as:

R. Álvarez, L. Aramburu, P. Puebla, E. Caballero, M. González, A. Vicente, M. Medarde, R. Peláez , Pyridine Based Antitumour Compounds Acting at the Colchicine Site, Current Medicinal Chemistry 2016; 23 (11) . https://dx.doi.org/10.2174/092986732311160420104823