title: Acylhydrazone derivatives as potential anticancer agents: Synthesis, bio-evaluation and mechanism of action.
abstract: A series of novel acylhydrazone derivatives were designed, synthesized and evaluated for their potential cytotoxic effects against human cancer cell lines. The preliminary results indicated that some of the obtained compounds (such as 8b, 13c) exhibited good to moderate cytotoxic activities against human HepG2, Huh-7, and BCG-823 cell lines. Especially, compounds 8c and 8e presented obviously selective cytotoxic activities against Huh-7 in vitro (8c, IC50=7.74±2.18μg/mL; 8e, IC50=4.46±1.05μg/mL) compared to 5-FU (IC50=10.41±3.41μg/mL). The highly potential compounds to induce apoptosis in HepG2 cells were analyzed by flow cytometry, and the apoptotic effects of compounds 8b and 13c were further evaluated using Annexin V-FITC/propidium iodide dual staining assay.
authors.affiliation: Huangshi Central Hospital, Hubei Polytechnic University, Huangshi 435000, People's Republic of China.
authors.forename: Xifang
authors.initials: X
authors.lastname: Yu
authors.affiliation: National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China.
authors.forename: Liqiao
authors.initials: L
authors.lastname: Shi
authors.affiliation: National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China. Electronic address: keshaoyong@163.com.
authors.forename: Shaoyong
authors.initials: S
authors.lastname: Ke
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D005472:Fluorouracil / Q000633:toxicity; D056945:Hep G2 Cells; D006801:Humans; D006835:Hydrazones / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity
chemical_list: D000970:Antineoplastic Agents; D006835:Hydrazones; D005472:Fluorouracil
keywords: Acylhydrazone; Apoptosis; Cytotoxic activity; Synthesis