Preparation and Antitumor Activity of a Tamibarotene-Furoxan Derivative
| Autor: | Tao Zhang, Yu Duan, Jin-Hong Feng, Li-Hong Shi, Xiu-Rong Zhang, Zong-Tao Li, Xiang-Po Pan, Xuejian Wang |
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| Rok vydání: | 2014 |
| Předmět: |
Drug
Cancer Research Tetrahydronaphthalenes Receptors Retinoic Acid Epidemiology media_common.quotation_subject Blotting Western Retinoic acid Mice Nude Antineoplastic Agents Pharmacology Nitric Oxide Benzoates Nitric oxide Mice chemistry.chemical_compound In vivo Tumor Cells Cultured Animals Humans Receptor Cell Proliferation media_common Ovarian Neoplasms Oxadiazoles Leukemia Drug discovery Furoxan Public Health Environmental and Occupational Health Xenograft Model Antitumor Assays Models Chemical Oncology chemistry Female Tamibarotene |
| Zdroj: | Asian Pacific Journal of Cancer Prevention. 15:6343-6347 |
| ISSN: | 1513-7368 |
| DOI: | 10.7314/apjcp.2014.15.15.6343 |
| Popis: | Multi-target drug design, in which drugs are designed as single molecules to simultaneously modulate multiple physiological targets, is an important strategy in the field of drug discovery. QT-011, a tamibarotene-furoxan derivative, was here prepared and proposed to exert synergistic effects on antileukemia by releasing nitric oxide and tamibarotene. Compared with tamibarotene itself, QT-011 displayed stronger antiproliferative effects on U937 and HL-60 cells and was more effective evaluated in a nude mice U937 xenograft model in vivo. In addition, QT-011 could release nitric oxide which might contribute to the antiproliferative activity. Autodocking assays showed that QT-011 fits well with the hydrophobic pocket of retinoic acid receptors. Taken together, these results suggest that QT-011 might be a highly effective derivative of tamibarotene and a potential candidate compound as antileukemia agent. |
| Databáze: | OpenAIRE |
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