title: Syntheses of novel β-carboline derivatives and the activities against five tumor-cell lines.
abstract: A series of β-carbolines possessing the aryl group at C-1 position has been synthesized from tryptophan. The newly synthesized compounds were screened for their in vitro anticancer activity against various human cancer cell lines by MTT assay. Some of them exhibited anticancer activity with IC50 values lower than 10μM outdistanced the cisplatin level. Structure-activity relationship reveals that the alcohol substituents at C-3 position played an important role in inhibition activity.
authors.affiliation: Chinese Center for Chirality, The Key Laboratory of Medicinal Chemistry and Molecular Diagnostics, Department of Chemistry and Chemical Engineering, Hebei University, Baoding 071002, China; School of Food and Biological Engineering, Zhengzhou University of Light Industry, Zhengzhou 450002, China.
authors.forename: Bing
authors.initials: B
authors.lastname: Bai
authors.affiliation: The State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, CAS, Kunming 650204, China.
authors.forename: Xing-Yao
authors.initials: XY
authors.lastname: Li
authors.affiliation: Chinese Center for Chirality, The Key Laboratory of Medicinal Chemistry and Molecular Diagnostics, Department of Chemistry and Chemical Engineering, Hebei University, Baoding 071002, China.
authors.forename: Li
authors.initials: L
authors.lastname: Liu
authors.affiliation: The State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, CAS, Kunming 650204, China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Li
authors.affiliation: Chinese Center for Chirality, The Key Laboratory of Medicinal Chemistry and Molecular Diagnostics, Department of Chemistry and Chemical Engineering, Hebei University, Baoding 071002, China; The State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, CAS, Kunming 650204, China. Electronic address: hjzhu@mail.kib.ac.cn.
authors.forename: Hua-Jie
authors.initials: HJ
authors.lastname: Zhu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002243:Carbolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D061986:MCF-7 Cells; D015394:Molecular Structure; D009369:Neoplasms / Q000473:pathology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D002243:Carbolines
keywords: Cytotoxic activity; MTT; Structure–activity relationship; β-Carbolines