Synthesis of novel ring-A fused hybrids of oleanolic acid with capabilities to arrest cell cycle and induce apoptosis in breast cancer cells
| Autor: | Vasant Naidu, Manish Kumar Jeengar, Nagi Reddy Vanga, Uppuluri V. Mallavadhani |
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| Rok vydání: | 2013 |
| Předmět: |
Male
Cell cycle checkpoint Magnetic Resonance Spectroscopy Apoptosis Breast Neoplasms Mass Spectrometry HeLa chemistry.chemical_compound Prostate Cell Line Tumor Drug Discovery medicine Humans MTT assay Oleanolic Acid skin and connective tissue diseases Oleanolic acid Pharmacology biology Chemistry Organic Chemistry Cell Cycle General Medicine Cell cycle biology.organism_classification Molecular biology medicine.anatomical_structure Biochemistry Cell culture |
| Zdroj: | European journal of medicinal chemistry. 74 |
| ISSN: | 1768-3254 |
| Popis: | Six novel oleanolic acid ring-A fused hybrids (5-10) have been synthesized by employing a four step protocol with the introduction of benzylidene functionality at C-2 as the key step. Their structures were established by high resolution NMR and Mass spectral data. The synthesized compounds have been screened against seven human cancer cell lines including ME-180 & HeLa (cervix), MCF-7, MDA-MB-453 & MDA-MB-231 (breast), PC-3 (prostate) and HT-29 (colon) using MTT assay. Most significantly, compound 10 showed potent activity against the three breast cancer cell lines. The IC₅₀ value (10.60 μM) of compound 10 against MCF-7 found to be much lower than that of the standards and parent compound. Flow cytometric analysis reveals that compound 10 arrests cell cycle in S phase and induces apoptosis in MCF cells. |
| Databáze: | OpenAIRE |
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