Tubulin polymerisation inhibitors that target colchicine binding site were powerful anticancer agents. Although along the years many colchicine binding site inhibitors (CBSIs) have been reported, few piperidine derivatives were identified as CBSIs. In this regard, we focussed efforts on the piperidine as a promising chemotype to develop potent CBSIs. Herein, novel piperidine derivatives were synthesised and evaluated for their antiproliferative activities. Among them, compound 17a displayed powerful anticancer activity with the IC50 value of 0.81 µM against PC3 cells, which was significantly better than 5-fluorouracil. It could inhibit tubulin polymerisation binding at the colchicine site and inhibit the tumour growth in vitro and in vivo. ...
International audienceStandard chemotherapies that interfere with microtubule dynamics are a chemoth...
We discovered a new chemical class of antiproliferative agents, 4-(1,2,4-oxadiazol-5-yl)piperidine-1...
Microtubules play critical roles in vital cell processes, including cell growth, division, and migra...
Microtubules are tubulin polymer structures, which are indispensable for cell growth and division. I...
A series of novel isocombretapyridines were designed and synthesized based on a lead compound isocom...
Colchicine, a natural product of Colchicum autumnae currently used for gout treatment, is a tubulin ...
Colchicine, a natural product of Colchicum autumnae currently used for gout treatment, is a tubulin ...
Specific modifications of colchicine followed by synthesis of its analogues have been tested in vitr...
International audienceColchicine, the main active alkaloid from Colchicum autumnale L., is a potent ...
We have developed a novel class (2-amino-4-phenyl-4H-chromene-3-carboxylate) of inhibitors of tubuli...
<div><p>Microtubules play critical roles in vital cell processes, including cell growth, division, a...
[[abstract]]P-glycoprotein (P-gp) is a drug transporter that effluxes chemotherapeutic drugs and is ...
Cancer is a genetic disease characterized by unregulated growth and dissemination of malignantly tra...
Natural products are a major source of anticancer agents and play critical roles in anticancer drug ...
We report the design, synthesis, and biological evaluation of heterocyclic-fused pyrimidines as tubu...
International audienceStandard chemotherapies that interfere with microtubule dynamics are a chemoth...
We discovered a new chemical class of antiproliferative agents, 4-(1,2,4-oxadiazol-5-yl)piperidine-1...
Microtubules play critical roles in vital cell processes, including cell growth, division, and migra...
Microtubules are tubulin polymer structures, which are indispensable for cell growth and division. I...
A series of novel isocombretapyridines were designed and synthesized based on a lead compound isocom...
Colchicine, a natural product of Colchicum autumnae currently used for gout treatment, is a tubulin ...
Colchicine, a natural product of Colchicum autumnae currently used for gout treatment, is a tubulin ...
Specific modifications of colchicine followed by synthesis of its analogues have been tested in vitr...
International audienceColchicine, the main active alkaloid from Colchicum autumnale L., is a potent ...
We have developed a novel class (2-amino-4-phenyl-4H-chromene-3-carboxylate) of inhibitors of tubuli...
<div><p>Microtubules play critical roles in vital cell processes, including cell growth, division, a...
[[abstract]]P-glycoprotein (P-gp) is a drug transporter that effluxes chemotherapeutic drugs and is ...
Cancer is a genetic disease characterized by unregulated growth and dissemination of malignantly tra...
Natural products are a major source of anticancer agents and play critical roles in anticancer drug ...
We report the design, synthesis, and biological evaluation of heterocyclic-fused pyrimidines as tubu...
International audienceStandard chemotherapies that interfere with microtubule dynamics are a chemoth...
We discovered a new chemical class of antiproliferative agents, 4-(1,2,4-oxadiazol-5-yl)piperidine-1...
Microtubules play critical roles in vital cell processes, including cell growth, division, and migra...