Discovery of FZU-03,010 as a self-assembling anticancer amphiphile for acute myeloid leukemia |
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Authors: | Yingyu Chen Cailong Li Yunquan Zheng Yu Gao Jianda Hu Haijun Chen |
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Affiliation: | 1. College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, China;2. Fujian Institute of Hematology, Fujian Provincial Key Laboratory of Hematology, Fujian Medical University Union Hospital, Fuzhou, Fujian 350001, China |
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Abstract: | Recently various drug candidates with excellent anticancer potency have been demonstrated, whereas their clinical application largely suffers from several limitations especially poor solubility. Ursolic acid (UA) as one of ubiquitous pentacyclic triterpenes in plant kingdom exhibited versatile antiproliferative effects in various cancer cell lines. However, the unfavorable pharmaceutical properties became the main obstacle for its clinical development. With the aim of development of novel derivatives with enhanced potency, a series of diversified UA amphiphiles have been designed, synthesized, and pharmacologically evaluated. Amphiphile 10 (FZU-03,010) with significant improved antiproliferative effect can self-assemble into stable nanoparticles in water, which may serve as a promising candidate for further development. |
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Keywords: | Ursolic acid Poor aqueous solubility Amphiphile Self-assembling Nanoparticles |
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