Synthesis of combretastatin A4 analogues on steroidal framework and their anti-breast cancer activity
| Autor: | Om Prakash, Arvind S. Negi, Bendangla Changkija, Amit K. Chaturvedi, Chandan S. Chanotiya, Feroz Khan, Murli Manohar, Karuna Shanker, Anila Dwivedi, Swati Parihar, Debabrata Chanda, Naresh Kumar Sachan, Rituraj Konwar, Amit Kumar, Suaib Luqman |
|---|---|
| Rok vydání: | 2012 |
| Předmět: |
Spectrometry
Mass Electrospray Ionization Magnetic Resonance Spectroscopy Endocrinology Diabetes and Metabolism medicine.medical_treatment Clinical Biochemistry Combretastatin a4 Breast Neoplasms Pharmacology Biochemistry Steroid Rats Sprague-Dawley chemistry.chemical_compound Mice Endocrinology Breast cancer Cell Line Tumor Stilbenes medicine Animals Humans Gallic acid skin and connective tissue diseases Cytotoxicity Molecular Biology Polymerase biology Chemistry Cell Biology medicine.disease Rats Docking (molecular) Apoptosis biology.protein Molecular Medicine Female Steroids |
| Zdroj: | The Journal of steroid biochemistry and molecular biology. 137 |
| ISSN: | 1879-1220 |
| Popis: | Combretastatin A4 analogues were synthesized on steroidal framework from gallic acid with a possibility of anti-breast cancer agents. Twenty two analogues were synthesized and evaluated for cytotoxicity against human breast cancer cell lines (MCF-7 & MDA-MB 231). The best analogue 22 showed potent antitubulin effect. Docking experiments also supported strong binding affinity of 22 to microtubule polymerase. In cell cycle analysis, 22 induced apoptosis in MCF-7 cells significantly. It was found to be non-toxic up to 300 mg/kg dose in Swiss albino mice in acute oral toxicity. This article is part of a Special Issue entitled “Synthesis and biological testing of steroid derivatives as inhibitors”. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect