title: Synthesis and antitumor activity of feruloyl and caffeoyl derivatives.
abstract: We developed two efficient protocols for the synthesis of feruloyl and caffeoyl derivatives from commercial vanillin and veratraldehyde. Pharmacological activities were assessed against a panel of human cancer cell lines in vitro. Most synthesized compounds demonstrated attractive cytotoxicity. Several new compounds demonstrated significant antiproliferative and cytotoxic activities against HeLa and Bewo tumor cell lines. In particular, 5-nitro caffeic adamantyl ester showed broad spectrum of tumor inhibition in 10 cell lines, and reduced tumor weight by 36.7% in vivo when administered at a dose of 40 mg kg(-1).
authors.affiliation: Sir Run Run Shaw Hospital, Zhejiang University, Hangzhou 310016, People's Republic of China.
authors.forename: Hui-Zhen
authors.initials: HZ
authors.lastname: Chen
authors.affiliation: College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, People's Republic of China.
authors.forename: You-Bao
authors.initials: YB
authors.lastname: Chen
authors.affiliation: College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, People's Republic of China.
authors.forename: Ya-Ping
authors.initials: YP
authors.lastname: Lv
authors.affiliation: College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, People's Republic of China.
authors.forename: Fang
authors.initials: F
authors.lastname: Zeng
authors.affiliation: College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, People's Republic of China.
authors.forename: Juan
authors.initials: J
authors.lastname: Zhang
authors.affiliation: Zhejiang Province People's Hospital, Hangzhou 310014, People's Republic of China.
authors.forename: Yong-Lie
authors.initials: YL
authors.lastname: Zhou
authors.affiliation: College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, People's Republic of China.
authors.forename: Han-Bing
authors.initials: HB
authors.lastname: Li
authors.affiliation: Zhejiang Hisun Pharmaceutical Co. Ltd., 46 Waisha Road, Jiaojiang District, Taizhou City, Zhejiang Province 318000, People's Republic of China.
authors.forename: Li-Fei
authors.initials: LF
authors.lastname: Chen
authors.affiliation: Ningbo Green-Health Pharmaceutical Co., Ltd, Fenghua Xiwu Town Foreign Technological Garden, Ningbo 315505, People's Republic of China.
authors.forename: Bin-Jie
authors.initials: BJ
authors.lastname: Zhou
authors.affiliation: College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, People's Republic of China.
authors.forename: Jian-Rong
authors.initials: JR
authors.lastname: Gao
authors.affiliation: College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, People's Republic of China. Electronic address: xcn77@zjut.edu.cn.
authors.forename: Chun-Nian
authors.initials: CN
authors.lastname: Xia
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002109:Caffeic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003373:Coumaric Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D002109:Caffeic Acids; D003373:Coumaric Acids; C004999:ferulic acid
keywords: Antitumor; Caffeoyl; Feruloyl; SARs