Syntheses and cytotoxicities of the analogues of the taxoid brevifoliol
| Autor: | J. Kotesh Kumar, Shubhra Negi, Brijesh S. Sisodia, Uzma Faridi, Sunil K. Chattopadhyay, Sarita Tripathi, Mahendra P. Darokar, Suman P. S. Khanuja |
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| Rok vydání: | 2007 |
| Předmět: |
Pharmacology
chemistry.chemical_classification Spectrometry Mass Electrospray Ionization Magnetic Resonance Spectroscopy Spectrophotometry Infrared Stereochemistry Carboxylic acid Organic Chemistry General Medicine Chemical synthesis Antineoplastic Agents Phytogenic Taxoid chemistry.chemical_compound chemistry Cell Line Tumor Drug Discovery Humans MTT assay Taxoids Diterpene Protecting group Cytotoxicity Enone |
| Zdroj: | European journal of medicinal chemistry. 43(7) |
| ISSN: | 0223-5234 |
| Popis: | Seven novel brevifoliol analogues have been synthesized by coupling brevifoliol and 2-monosubstituted-4-phenyl-1,3-oxazolidine carboxylic acid after removal of the protecting group with acid treatment. Brevifoliol and its synthesized analogues were tested for their cytotoxic activities against four different human cancer cell lines, oral (KB), breast (MCF-7), colon (CaCO2) and liver (HepG-2) as determined by MTT assay. The C-13 oxidized brevifoliol retained significant activity. Out of the seven analogues synthesized, C-13 oxidized brevifoliol-5-[N-tert-butoxycarbonyl amino-(2'R,3'S)-3'-phenyl isoserine] analogue was interesting as it exhibited selective and potent cytotoxicity against liver cancer cell line predominantly. |
| Databáze: | OpenAIRE |
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