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Synthesis and biological evaluation of novel anticancer bivalent colchicine-tubulizine hybrids.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2012 Jul 15; Vol. 20 (14), pp. 4271-8. Date of Electronic Publication: 2012 Jun 06. - Publication Year :
- 2012
-
Abstract
- A series of novel antimitotic hybrids were synthesized in good yields by linking of azide-containing colchicine congeners with acetylene-substituted tubulizine-type derivatives using copper-mediated 1,3-dipolar cycloaddition. Obtained compounds exhibit good cytotoxicity against HBL100 epithelial cell lines (IC(50)=0.599-2.93 μМ). Several newly synthesized compounds are the substoichiometric inhibitors of microtubule assembly (R=0.41-0.78). The results highlight the importance of the length of spacer linking the tubulin binding ligands in heterodimeric molecules.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antineoplastic Agents chemistry
Antineoplastic Agents toxicity
Cell Line
Cell Survival drug effects
Click Chemistry
Colchicine chemical synthesis
Colchicine chemistry
Colchicine toxicity
Dimerization
Humans
Ligands
Microtubules metabolism
Protein Binding
Tubulin Modulators chemistry
Tubulin Modulators toxicity
Antineoplastic Agents chemical synthesis
Colchicine analogs & derivatives
Microtubules chemistry
Tubulin Modulators chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 20
- Issue :
- 14
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 22739088
- Full Text :
- https://doi.org/10.1016/j.bmc.2012.05.072