Synthesis and Biological evaluation of novel 4β-[(5-substituted)-1,2,3,4-tetrazolyl] podophyllotoxins as anticancer compounds
| Autor: | Halmuthur M. Sampath Kumar, Naresh Nalla, Deepthi Yedlapudi, Irfan Hyder, Sreekanth Miryala, Jabeena Khazir, Shasi V. Kalivendi, Tabasum Ismail |
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| Rok vydání: | 2014 |
| Předmět: |
Stereochemistry
Cell Survival Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Biochemistry Structure-Activity Relationship Tubulin Cell Line Tumor Drug Discovery medicine Tubulin polymerization Humans Doxorubicin Cytotoxicity Molecular Biology Biological evaluation Podophyllotoxin Chemistry Organic Chemistry Cell Cycle Checkpoints In vitro Tubulin Modulators Cell culture Click chemistry Molecular Medicine Human cancer medicine.drug HeLa Cells |
| Zdroj: | Bioorganicmedicinal chemistry letters. 25(14) |
| ISSN: | 1464-3405 |
| Popis: | A series of novel 4β-[(5-substituted)-1,2,3,4-tetrazolyl] podophyllotoxin derivatives were synthesized by employing azide-nitrile click chemistry approach. All the derivatives were evaluated for their cytotoxicity against a panel of four human cancer cell lines and their IC 50 values were found to be in the range of 2.4–29.06 μM. The cytotoxicity exhibited by the majority of test compounds were found to comparable and often more effective than doxorubicin and all compounds exhibited higher cytotoxicity on A-549 cell lines. Cell cycle analysis showed that the novel 4β-[(5-substituted)-1,2,3,4-tetrazolyl] podophyllotoxins resulted in cell cycle arrest at G2/M phase and were also found to be the potent inhibitors of tubulin polymerization in vitro. |
| Databáze: | OpenAIRE |
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