Synthesis and cytotoxicity of (-)-renieramycin G analogs
| Autor: | Nan Wang, Wei Liu, Baohe Guan, Zhanzhu Liu, Zheng Yan, Wenfang Dong, Xiangwei Liao |
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| Rok vydání: | 2010 |
| Předmět: |
Stereochemistry
Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Biochemistry Chemical synthesis HeLa chemistry.chemical_compound Inhibitory Concentration 50 Structure-Activity Relationship Cell Line Tumor Tetrahydroisoquinolines Drug Discovery Structure–activity relationship Humans Tyrosine Cytotoxicity Molecular Biology IC50 Cell Proliferation biology Organic Chemistry biology.organism_classification In vitro chemistry Lactam Molecular Medicine HeLa Cells |
| Zdroj: | Bioorganicmedicinal chemistry letters. 21(5) |
| ISSN: | 1464-3405 |
| Popis: | (−)-Renieramycin G and fifteen C-22 analogs were prepared employing l -tyrosine as the chiral starting material. These analogs, along with (−)-renieramycin G itself, were evaluated in vitro for cytotoxicity against HCT-8, BEL-7402, A2780, MCF-7, A549, BGC-823, Ketr3, KB, Hela cells. The IC50 values of most of these analogs were at the level of μM. Among these analogs, 2-thiophenecarboxylate ester derivative 17 exhibited potent cytotoxic activity against KB cell line with the IC50 of 20 nM. From this study, it could be concluded that the C-22 side chain played an important role in the cytotoxic potency and specificity of this class of (−)-renieramycin G derivatives. |
| Databáze: | OpenAIRE |
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