Design and synthesis of taxane derivatives of valproic acid as potent and selective cytotoxic agents
| Autor: | Himaja Malipeddi, Moonjit Das, Sunil V. Mali |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Valproic Acid Taxane Organic Chemistry Drug resistance Pharmacology 03 medical and health sciences chemistry.chemical_compound 030104 developmental biology 0302 clinical medicine Paclitaxel chemistry Docetaxel 030220 oncology & carcinogenesis Cancer cell medicine Moiety General Pharmacology Toxicology and Pharmaceutics Cytotoxicity medicine.drug |
| Zdroj: | Medicinal Chemistry Research. 25:2512-2520 |
| ISSN: | 1554-8120 1054-2523 |
| DOI: | 10.1007/s00044-016-1635-6 |
| Popis: | Resistance to anticancer agents has important implications for cancer chemotherapy. Small changes in chemical structures of cytotoxic agents can alter their biological interactions that can be beneficial in overcoming the drug resistance problem. Valproic acid, a well-known antiepileptic drug is in advanced clinical studies for cancer treatment. In the present study, valproic acid was incorporated into the taxane moiety at various positions and the new analogs were evaluated for their in vitro cytotoxicity. The novel analog, Valprotaxel showed comparable cytotoxicity in head and neck, and colon cancer cell lines with remarkable improvement in selectivity for cancer cells compared to paclitaxel and docetaxel. |
| Databáze: | OpenAIRE |
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