title: Discovery of FZU-03,010 as a self-assembling anticancer amphiphile for acute myeloid leukemia.
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.
authors.affiliation: 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.
authors.forename: Yingyu
authors.initials: Y
authors.lastname: Chen
authors.affiliation: College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, China.
authors.forename: Cailong
authors.initials: C
authors.lastname: Li
authors.affiliation: College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, China.
authors.forename: Yunquan
authors.initials: Y
authors.lastname: Zheng
authors.affiliation: College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Gao
authors.affiliation: Fujian Institute of Hematology, Fujian Provincial Key Laboratory of Hematology, Fujian Medical University Union Hospital, Fuzhou, Fujian 350001, China. Electronic address: drjiandahu@163.com.
authors.forename: Jianda
authors.initials: J
authors.lastname: Hu
authors.affiliation: College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, China. Electronic address: chenhaij@gmail.com.
authors.forename: Haijun
authors.initials: H
authors.lastname: Chen
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D055808:Drug Discovery; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006801:Humans; D015470:Leukemia, Myeloid, Acute / Q000473:pathology*; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; C000621943:FZU-03,010; D010879:Piperazines; D014315:Triterpenes
keywords: Amphiphile; Nanoparticles; Poor aqueous solubility; Self-assembling; Ursolic acid