Synthesis and antitumor evaluation of methyl spongoate analogs
| Autor: | Jing-Xu Gong, Cheng-Shi Jiang, Jia Li, Bo Feng, Tibor Kurtán, Cai-Guo Huang, Yue-Wei Guo |
|---|---|
| Rok vydání: | 2010 |
| Předmět: |
Pharmacology
Stereochemistry Organic Chemistry Clinical Biochemistry Antineoplastic Agents Biochemistry In vitro Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Endocrinology Biosynthesis chemistry Cell Line Tumor Michael reaction Side chain Humans Cytotoxic T cell Moiety Steroids Methyl spongoate Cytotoxicity Molecular Biology |
| Zdroj: | Steroids. 75:1153-1163 |
| ISSN: | 0039-128X |
| DOI: | 10.1016/j.steroids.2010.08.002 |
| Popis: | A series of novel methyl spongoate (1) analogs has been synthesized and evaluated for their in vitro cytotoxic properties. It was found that the nature of the C-20 side chain had significant effects on their bioactivities and some analogs showed higher cytotoxicity than 1 against A549, HCT-116, HepG2, SW-1990, MCF-7 and NCI-H460 tumor cell lines. The pharmacological results confirmed that the α,β-unsaturated carbonyl moiety, a Michael acceptor in ring A, plays a pivotal role in the cytotoxic effect of these derivatives. The compiled pharmacological data may be useful for the design of novel analogous anticancer drugs. |
| Databáze: | OpenAIRE |
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