title: Synthesis, antitumor activity evaluation of some new N-aroyl-α,β-unsaturated piperidones with fluorescence.
abstract: Novel N-aroyl-α,β-unsaturated piperidones, series 1, series 2 and series 3 (featuring 2-bromo-4,5-dimethoxybenzylidene, 4-dimethylaminobenzylidene and 4-trifluoromethylbenzylidene, respectively), were synthesized as candidate cytotoxins. Most of the compounds displayed potent cytotoxicity against the human neoplastic cell lines SK-BR-3, PG-BE1, NCI-H460, MIA PaCa-2 and SW1990 in vitro, and approximately 64% of the IC50 values were lower than 5 μM. Among those tested, compound 1b of series 1, 3a, 3d and 3e of series 3 proved to be the most active. Importantly, 1b displayed marked inhibitory effects on tumor growth in vivo and had no apparent toxicity to mice; this was evaluated by a nude mouse PG-BE1 xenograft model. In addition, the fluorescent properties of compounds series 1-3 were investigated. The interesting fluorescence exhibited by these compounds could be useful for their visualization in tumor cells, permitting further studies on these α,β-unsaturated piperidones as candidates for novel fluorescent antitumor agents.
authors.affiliation: a 1 School of Pharmacy, Binzhou Medical University , Yantai , Shandong , P.R. China and.
authors.forename: Jufeng
authors.initials: J
authors.lastname: Sun
authors.affiliation: b 2 Yantai Yuhuangding Hospital Emergency , Yantai , Shandong , P.R. China.
authors.forename: Suwen
authors.initials: S
authors.lastname: Wang
authors.affiliation: a 1 School of Pharmacy, Binzhou Medical University , Yantai , Shandong , P.R. China and.
authors.forename: Hongjuan
authors.initials: H
authors.lastname: Li
authors.affiliation: a 1 School of Pharmacy, Binzhou Medical University , Yantai , Shandong , P.R. China and.
authors.forename: Wenguo
authors.initials: W
authors.lastname: Jiang
authors.affiliation: a 1 School of Pharmacy, Binzhou Medical University , Yantai , Shandong , P.R. China and.
authors.forename: Guige
authors.initials: G
authors.lastname: Hou
authors.affiliation: a 1 School of Pharmacy, Binzhou Medical University , Yantai , Shandong , P.R. China and.
authors.forename: Feng
authors.initials: F
authors.lastname: Zhao
authors.affiliation: a 1 School of Pharmacy, Binzhou Medical University , Yantai , Shandong , P.R. China and.
authors.forename: Wei
authors.initials: W
authors.lastname: Cong
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D005453:Fluorescence; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D015394:Molecular Structure; D009374:Neoplasms, Experimental / Q000188:drug therapy / Q000473:pathology; D010881:Piperidones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D010881:Piperidones
keywords: Antitumor agents; cytotoxicity; fluorescence; xenograft model; α,β-unsaturated piperidones