Pyridine Based Antitumour Compounds Acting at the Colchicine Site

被引：42

作者：

Alvarez, R.

Aramburu, L.

Puebla, P.

Caballero, E.

Gonzalez, M.

Vicente, A.

Medarde, M.

Pelaez, R.

机构：

[1] Univ Salamanca, Fac Farm, CIETUS Ctr Enfermedades Trop, Lab Quim Org & Farmaceut, Campus Miguel de Unamuno, E-37007 Salamanca, Spain

[2] Univ Salamanca, IBSAL Inst Invest Biomed Salamanca, Campus Miguel de Unamuno, E-37007 Salamanca, Spain

来源：

CURRENT MEDICINAL CHEMISTRY | 2016年 / 23卷 / 11期

关键词：

Pyridine; azines; antimitotics; tubulin; colchicine; antitumour; drug design; PHASE-II TRIAL; TUBULIN-POLYMERIZATION INHIBITORS; VASCULAR-DISRUPTING AGENTS; ALPHA-BETA-TUBULIN; CELL LUNG-CANCER; HYDROGEN-BOND BASICITY; TIVANTINIB ARQ 197; BIOLOGICAL EVALUATION; IN-VITRO; ANTIMITOTIC AGENTS;

D O I：

10.2174/092986732311160420104823

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

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.

引用

页码：1100 / 1130

页数：31

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