2. Academic Validation
  3. Discovery of FZU-03,010 as a self-assembling anticancer amphiphile for acute myeloid leukemia

Discovery of FZU-03,010 as a self-assembling anticancer amphiphile for acute myeloid leukemia

  • Bioorg Med Chem Lett. 2017 Feb 15;27(4):1007-1011. doi: 10.1016/j.bmcl.2016.12.071.
Yingyu Chen 1,  Cailong Li 2,  Yunquan Zheng 2,  Yu Gao 2,  Jianda Hu 3,  Haijun Chen 4
Affiliations

Affiliations

  • 1 College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, China; Fujian Institute of Hematology, Fujian Provincial Key Laboratory of Hematology, Fujian Medical University Union Hospital, Fuzhou, Fujian 350001, China.
  • 2 College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, China.
  • 3 Fujian Institute of Hematology, Fujian Provincial Key Laboratory of Hematology, Fujian Medical University Union Hospital, Fuzhou, Fujian 350001, China. Electronic address: drjiandahu@163.com.
  • 4 College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, China. Electronic address: chenhaij@gmail.com.
PMID: 28073673 DOI: 10.1016/j.bmcl.2016.12.071
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 plantkingdom 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.

Keywords

Amphiphile; Nanoparticles; Poor aqueous solubility; Self-assembling; Ursolic acid.

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