Exploring the size adaptability of the B ring binding zone of the colchicine site of tubulin with para-nitrogen substituted isocombretastatins

We have synthesized and assayed dimethylaminophenyl, pyrrolidin-1-ylphenyl and carbazole containing phenstatins and isocombretastatins as analogues of the highly potent indoleisocombretastatins with extended or reduced ring sizes. This is an attempt to explore beyond the structural constraints of th...

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Veröffentlicht in:	European journal of medicinal chemistry 2015-07, Vol.100, p.210-222
Hauptverfasser:	Jiménez, Carmen, Ellahioui, Younes, Álvarez, Raquel, Aramburu, Laura, Riesco, Alejandra, González, Myriam, Vicente, Alba, Dahdouh, Abdelaziz, Ibn Mansour, Ahmed, Jiménez, Carlos, Martín, Diego, Sarmiento, Rogelio G., Medarde, Manuel, Caballero, Esther, Peláez, Rafael
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Autophagy Binding Sites - drug effects Cell Cycle - drug effects Cell Line, Tumor Cell Proliferation - drug effects Colchicine - chemical synthesis Colchicine - chemistry Colchicine - pharmacology Cytotoxicity Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Humans Isocombretastatins Models, Molecular Molecular Structure Nitrogen - chemistry para-Nitrogen-substituted Particle Size Phenstatins Stilbenes - chemistry Stilbenes - pharmacology Structure-Activity Relationship Tubulin - chemistry Tubulin - metabolism Tubulin polymerization inhibition
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