title: Synthesis, biological evaluation and SAR analysis of O-alkylated analogs of quercetin for anticancer.
abstract: O-Alkylated quercetin analogs were synthesized and their anticancer activities were assessed by a high-throughout screening (HTS) method. The structure-activity relationships (SAR) showed that introduction of long alkyl chain such as propyl group at the C-3 OH position or short alkyl chain such as ethyl group at the C-4' OH position were very important for keeping inhibitory activities against the 16 cancer cell lines. Furthermore, when the two n-butyl groups were introduced into the C-3, C-7 or C-4', C-7 positions, the anticancer activity was enhanced.
authors.affiliation: National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China; Department of Organic Chemistry, China Pharmaceutical University, Nanjing, Jiangsu 211198, China.
authors.forename: Zhi-Hao
authors.initials: ZH
authors.lastname: Shi
authors.affiliation: National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China. Electronic address: linianguang@njutcm.edu.cn.
authors.forename: Nian-Guang
authors.initials: NG
authors.lastname: Li
authors.affiliation: National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China. Electronic address: yupingtang@njutcm.edu.cn.
authors.forename: Yu-Ping
authors.initials: YP
authors.lastname: Tang
authors.affiliation: National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China.
authors.forename: Qian-Ping
authors.initials: QP
authors.lastname: Shi
authors.affiliation: National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Zhang
authors.affiliation: National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China.
authors.forename: Peng-Xuan
authors.initials: PX
authors.lastname: Zhang
authors.affiliation: National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China.
authors.forename: Ze-Xi
authors.initials: ZX
authors.lastname: Dong
authors.affiliation: National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Li
authors.affiliation: National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China.
authors.forename: Xu
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Department of Pharmacology, Emory University School of Medicine, Atlanta, GA 30322, United States.
authors.forename: Hai-An
authors.initials: HA
authors.lastname: Fu
authors.affiliation: National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China. Electronic address: dja@njutcm.edu.cn.
authors.forename: Jin-Ao
authors.initials: JA
authors.lastname: Duan
mesh_terms: D000478:Alkylation; 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; D006367:HeLa Cells; D057166:High-Throughput Screening Assays; D006801:Humans; D015394:Molecular Structure; D011794:Quercetin / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D011794:Quercetin
keywords: Alkylation; Anticancer; Quercetin; Structure–activity relationship