Design and synthesis of taxane derivatives of valproic acid as potent and selective cytotoxic agents
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...
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| Veröffentlicht in: | Medicinal chemistry research 2016-11, Vol.25 (11), p.2512-2520 |
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| container_title | Medicinal chemistry research |
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| creator | Malipeddi, Himaja Mali, Sunil V. Das, Moonjit |
| description | 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. |
| doi_str_mv | 10.1007/s00044-016-1635-6 |
| format | Article |
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| ispartof | Medicinal chemistry research, 2016-11, Vol.25 (11), p.2512-2520 |
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| language | eng |
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| subjects | Acid resistance Antiepileptic agents Antitumor agents Biochemistry Biomedical and Life Sciences Biomedicine Cell Biology Chemical synthesis Chemotherapy Colon cancer Cytotoxic agents Cytotoxicity Drug resistance Head & neck cancer Original Research Paclitaxel Pharmacology/Toxicology Taxanes Toxicity Tumor cell lines Valproic acid |
| title | Design and synthesis of taxane derivatives of valproic acid as potent and selective cytotoxic agents |
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