title: Antiproliferative activity and SARs of caffeic acid esters with mono-substituted phenylethanols moiety.
abstract: A series of CAPE derivatives with mono-substituted phenylethanols moiety were synthesized and evaluated by MTT assay on growth of 4 human cancer cell lines (Hela, DU-145, MCF-7 and ECA-109). The substituent effects on the antiproliferative activity were systematically investigated for the first time. It was found that electron-donating and hydrophobic substituents at 2'-position of phenylethanol moiety could significantly enhance CAPE's antiproliferative activity. 2'-Propoxyl derivative, as a novel caffeic acid ester, exhibited exquisite potency (IC50=0.4±0.02 & 0.6±0.03μM against Hela and DU-145 respectively).
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
authors.forename: Jin
authors.initials: J
authors.lastname: Xie
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
authors.forename: Fengzhi
authors.initials: F
authors.lastname: Yang
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
authors.forename: Man
authors.initials: M
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
authors.forename: Celine
authors.initials: C
authors.lastname: Lam
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
authors.forename: Yixue
authors.initials: Y
authors.lastname: Qiao
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
authors.forename: Jia
authors.initials: J
authors.lastname: Xiao
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
authors.forename: Dongdong
authors.initials: D
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
authors.forename: Yuxuan
authors.initials: Y
authors.lastname: Ge
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China. Electronic address: leifu@sjtu.edu.cn.
authors.forename: Lei
authors.initials: L
authors.lastname: Fu
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China. Electronic address: dshxie@sjtu.edu.cn.
authors.forename: Dongsheng
authors.initials: D
authors.lastname: Xie
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002109:Caffeic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004952:Esters / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D010626:Phenylethyl Alcohol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: C000622939:2'-propoxyphenethyl 3-(3,4-dihydroxyphenyl)acrylate; D000970:Antineoplastic Agents; D002109:Caffeic Acids; D004952:Esters; D010626:Phenylethyl Alcohol
keywords: Antiproliferative activity; CAPE derivatives; Caffeic acid esters; Structure-activity relationships